162 results on '"KHAN, KHALID"'
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2. Heavy Metal Resistant Bacteria from Soil as Potential Bioremediation Targets: Isolation, Screening andamp; Biochemical Identification
- Author
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Khalid Khan and Zahid Khan, Khalid Khan and Zahid Khan, primary
- Published
- 2021
- Full Text
- View/download PDF
3. Synthesis, Spectral Evaluation and in Silico Studies of S-Aralkylated 5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazole-3-thiols: As suitable Alzheimerand#39;s disease drug candidates
- Author
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Muhammad Arfan, Muhammad Arfan, primary, Sabahat Zahra Siddiqui, Sabahat Zahra Siddiqui, additional, Muhammad Athar Abbasi, Muhammad Athar Abbasi, additional, Aziz ur Rehman, Aziz ur Rehman, additional, Syed Adnan Ali Shah, Syed Adnan Ali Shah, additional, Muhammad Ashraf, Muhammad Ashraf, additional, Khalid Mohammed Khan, Khalid Mohammed Khan, additional, and Rahman Shah Zaib Saleem and Amna Shah Zaib, Rahman Shah Zaib Saleem and Amna Shah Zaib, additional
- Published
- 2021
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- View/download PDF
4. Synthesis, Characterization and Cytotoxic Effect of Some New Thiazolyl Hydrazone Derivatives of 1-Indanone
- Author
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Urooj Nazim, Urooj Nazim, primary, Silpa Narayanan, Silpa Narayanan, additional, Mohsin Ali, Mohsin Ali, additional, Khalid Mohammed Khan, Khalid Mohammed Khan, additional, Basharat Ali, Basharat Ali, additional, Jonathan Li, Jonathan Li, additional, Zhe Sheng Chen, Zhe Sheng Chen, additional, and Mansoor Ahmed and Dong Hua Yang, Mansoor Ahmed and Dong Hua Yang, additional
- Published
- 2021
- Full Text
- View/download PDF
5. Synthesis, Spectral Evaluation and in Silico Studies of S-Aralkylated 5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazole-3-thiols: As suitable Alzheimer's disease drug candidates.
- Author
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Arfan, Muhammad, Siddiqui, Sabahat Zahra, Abbasi, Muhammad Athar, Aziz-ur-Rehman, Shah, Syed Adnan Ali, Ashraf, Muhammad, Khan, Khalid Mohammed, Saleem, Rahman Shah Zaib, and Zaib, Amna Shah
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ALZHEIMER'S disease ,APROTIC solvents ,BENZYLIC group ,POLAR solvents ,PSEUDOPOTENTIAL method ,ACETYLCHOLINESTERASE - Abstract
Our efforts lay emphasis on synthesis of S-aralkylated 5-(4-OMeC6H5)-4-phenyl-4H-1,2,4-triazol-3-thiols like pharmacologically active candidates to counter neurodegenerative disorder; Alzheimer's disease. A synthetic strategy was instigated by esterifying 4-methoxybenzoic acid through Fisher esterification's methodology. Hydrazinolysis of corresponding ester was performed under reflux with methanolic hydrated hydrazine to afford 4-methoxybenzohydrazide (I) which refluxing with phenyl isothiocyanate (II) in MeOH to yield a reactive intermediate (III). The later underwent base-catalyzed intermolecular cyclization to furnish 5-(4-OMeC
6 H5 )-4H-1,2,4-triazol-3-thiol (IV). Ultimately, IV was aralkylated at thiol position with aralkyl halides V(a-l) in polar aprotic solvent and catalytic amounts of LiH to provide S-aralkylated 5-(4-OMeC6 H5 )-4-phenyl-4H-1,2,4-triazol-3-thiols VI(a-l). Modern spectral analysis data explicitly established all the substitutions on nucleophilic S-atom of parent 1,2,4-triazol-3-thiol ring. Effective anti-cholinesterase potential depicted in 3-(phenylpropylthio)-5-(4-OMeC6 H5 )-4-phenyl-4H-1,2,4-triazole; VIc (IC50; 3.26±0.35 µM) against acetyl cholinesterase; AChE and 3-(phenethylthio)-5-(4-OMeC6H5)-4-phenyl-4H-1,2,4-triazole; VIb (IC50 ; 8.52±0.54 µM) against butyrylcholinesterase; BChE enzyme as compared to standard Eserine for both enzymes (IC50 ; 0.04±0.01 µM). Molecular modelling analyses had been conducted to recognize the interconnection of these compounds with enzymes that suggested key interactions (Docking is made to untie the active binding sites). Anti-proliferative activity results showed VIg and VIj with -Cl groups on benzylic ring as promising candidates with HCT-116 cell viability of 14.83 % and 3.09 % respectively. [ABSTRACT FROM AUTHOR]- Published
- 2021
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6. Synthesis of Nʹ-Nicotinoyl Sulfonohydrazides and their Antimicrobial Activity
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Zarina Arshad, Zarina Arshad, primary, Sumayya Saied, Sumayya Saied, additional, Basharat Ali, Basharat Ali, additional, Uzma Salar, Uzma Salar, additional, Saima Tauseef, Saima Tauseef, additional, Arshia, Arshia, additional, Munazza Ajaz, Munazza Ajaz, additional, Uroosa Khan, Uroosa Khan, additional, Syed Moazzam Haider, Syed Moazzam Haider, additional, Muhammad Taha, Muhammad Taha, additional, and Khalid Mohammed Khan, Khalid Mohammed Khan, additional
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- 2020
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7. Phytochemical Analysis and Anthelmintic Activity of Salsola imbricata
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Muhammad Ajaib, Muhammad Ajaib, primary, Saleha Farooq, Saleha Farooq, additional, Khalid Mohammed Khan, Khalid Mohammed Khan, additional, and Shahnaz Perveen and Shazia Shah, Shahnaz Perveen and Shazia Shah, additional
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- 2019
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8. Synthetic 4,4'-{(Arylmethylene)}bis(1H-pyrazol-5-ols): Efficient Radical Scavengers.
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Qurat-ul-ain, Perveen, Shahida, Muhammad, Munira Taj, Yousuf, Sahar, Khan, Khalid Mohammed, and Choudhary, M. Iqbal
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PYRAZOLES ,ANTIOXIDANTS ,IN vitro studies ,CHEMICAL synthesis ,NAPHTHALENE derivatives - Abstract
Functionalized 4,4'-{(arylmethylene)}bis(1H-pyrazol-5-ols) 1-22 were screened for their antioxidant activity. Antioxidant activity was performed by measuring their radical scavenging activity. These compounds demonstrated diverse in vitro DPPH radical scavenging activities with IC
50 values ranging between 55.2 ± 1.2-149.6 ± 1.7 μM, as compared to standard BHT (butylated hydroxytoluene) (IC50 = 128.8 ± 2.1 μM). Compounds 4,4'-((4-bromo-2,6- dimethoxyphenyl)methylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ol 18) IC50 = 55.2 ± 1.2 μM, 4,4'- (naphthalen-1-ylmethylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ol 20) (IC50 = 58.3 ± 0.9 μM), 4,4'- ((3-bromo-4-methoxyphenyl)methylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ol 19) (IC50 = 59.6 ± 0.1 μM), 4,4'-((4-methoxyphenyl)methylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ol 6) (IC50 = 60.01 ± 0.7 μM), 4,4'-((4-(methylthio)phenyl)methylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ol 10) (IC50 = 61.5 ± 0.6 μM), 4,4'-((2,4-dimethylphenyl)methylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ol) (1) (IC50 = 68.3 ± 0.2 μM), 4,4'-((2-ethoxyphenyl)methylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ol) (8) (IC50 = 80.5 ± 1.5 μM), 4,4'-((3-nitrophenyl)methylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ol) (12) (IC50 = 70.8 ± 1.4 μM), 4,4'-((3-bromophenyl)methylene)bis(3-methyl-1-phenyl-1H-pyrazol-5- ol) (17) (IC50 = 77.9 ± 2.06 μM), and 4,4'-((2-fluorophenyl)methylene)bis(3-methyl-1-phenyl-1Hpyrazol- 5-ol) (22) (IC50 80.0 ± 2.3 μM) showed better antioxidant activity than the standard BHT. Varying substituents at aryl part (aldehydic part) have been responsible for diversified activity. [ABSTRACT FROM AUTHOR]- Published
- 2018
9. Application of Acid Dyes on Silk Fabric and Fastness Properties Part II.
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Akhtar, Zeeshan, Ali, Syed Imran, Farooq, Muhammad, Zubair, Salman, Parveen, Rasheeda, and Khan, Khalid M.
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ACID dyeing (Textiles) ,SILK ,COLORFASTNESS (Textiles) ,INFRARED spectroscopy ,NUCLEAR magnetic resonance spectroscopy - Abstract
Synthesis of acid dyes was carried out by reacting diazotized substituted aryl amines and substituted naphthalene sulfonic acid as coupling component. Structural properties were studied by UV-visible spectroscopy, IR spectroscopy,
1 H-NMR spectroscopy, MALDI-TOF mass spectrometric analysis and elemental analysis. Application of dyes was carried out on silk fabric and their fastness to light, washing, perspiration, and crocking was determined. The results revealed that the synthesized dyes are efficient for dyeing silk fabric which is evident from their excellent fixation, binding stability and fastness properties. [ABSTRACT FROM AUTHOR]- Published
- 2018
10. Alkali Hydrolyzed Conversion of Fish Scales into Protein Hydrolysates and Evaluation of their Antimicrobial Activity against Different Pathogenic Bacteria.
- Author
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Hussain, Zahid, Rafiq, Nasim, Niaz, Sadaf, Mohammed Khan, Khalid, Dil, Sobia, Perveen, Zahida, Mabood, Fazal, Jabeen, Farah, and Ara, Husan
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PROTEIN hydrolysates ,ANTI-infective agents ,FOURIER transform infrared spectroscopy ,SODIUM hydroxide ,BACTERIAL genetics ,ESCHERICHIA coli ,ESCHERICHIA coli mutation - Abstract
In this study the fish scales a waste product from the fish industry were converted into water soluble protein hydrolysates on heating with aqueous solution of sodium hydroxide. Those protein hydrolysates were fractionated into different fractions using solvent extraction procedure and were also checked for their antibacterial activity using agar well diffusion method. Their antibacterial activity was also tested against six pathogenic bacteria including Escherichia coli, Margenella morganii, Haemophilus influenzae, Klebsilla pneumoniae, Pseudomonas aeruginosa, and Actenobactor baumannii. All fractions were found active against these bacteria. Their zones of inhibitions were found to vary according to the nature of solvent fraction and bacteria. Maximum zones were observed for ethyl acetate fraction (neutral) against Escherichia coli and Actenobactor baumannii with zone of inhibition 19.5 mm and 17.0 mm, respectively almost equal to the control. Their chemical composition was also analyzed by using FTIR spectroscopy and spot test. These fractions and crude were found containing amides, amino acids, amines, phenols, alcohols and aldehydes functional groups. Their antibacterial activity was then correlated with their chemical composition along with their determination for percent yield and percentage of extraction. [ABSTRACT FROM AUTHOR]
- Published
- 2017
11. Anti-inflammatory Activity of 3-Thiazolyl Coumarins.
- Author
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Salar, Uzma, Khan, Khalid Mohammed, Jabeen, Almas, Bakhtawar, Faheem, Aisha, Taha, Muhammad, Ali, Farman, Syed, Shazia, Kanwal, Haider, Syed Moazzam, and Perveen, Shahnaz
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ANTI-inflammatory agents , *COUMARINS , *ZYMOSAN , *PHAGOCYTES , *CHEMILUMINESCENCE - Abstract
3-Thiazolyl coumarins 1-33 along with coumarin scaffold (IC50 = 5.2 ± 0.2 µg/mL) were evaluated for in vitro antiinflammatory activity. Activity of compounds was investigated by looking their influence on oxidative burst activity of zymosan stimulated whole blood phagocytes by using a luminol enhanced chemiluminescence technique. Ibuprofen was used as standard drug (IC50 = 54.2 ± 9.2 µM). Four 3-thiazolyl coumarin derivatives 9 (IC50 = 31.0 ± 2.5 µg/mL), 13 (IC50 = 27.1 ± 4.2 µg/mL), 18 (IC50 = 5.6 ± 2.6 µg/mL), and 29 (IC50 = 1.9 ± 1.0 µg/mL) out of thirty-three demonstrated antiinflammatory activity as compared to the standard ibuprofen (IC50 = 11.2 ± 1.9 µg/mL). Especially, compound 29 showed many folds better activity as compared to coumarin and standard ibuprofen. Structure-activity relationship was also established. It is worth-mentioning that active analogs 9, 13, 18, and 29 were found to be non-toxic on NIH-3T3 mouse fibroblast cell line. [ABSTRACT FROM AUTHOR]
- Published
- 2017
12. Anti-Leishmanial Activities of Synthetic Biscoumarins.
- Author
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Rahim, Fazal, Samreen, Ullah, Hayat, Fakhri, Muhammad Imran, Salar, Uzma, Perveen, Shahnaz, Khan, Khalid Mohammed, and Choudhary, M. Iqbal
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AMASTIGOTES ,PENTAMIDINE ,ANTIFUNGAL agents ,TOXICITY testing ,SULFONES - Abstract
Synthetic biscoumarins 1-19 were screened to check their anti-leishmanial activity. Out of nineteen, analogs 2 (IC
50 = 46.95 ± 1.23 μM), 4 (IC50 = 63.03 ± 0.20 μM), 5 (IC50 = 41.35 ± 0.51 μM), 6 (IC50 = 35.62 ± 0.15 μM), 7 (IC50 = 75.35 ± 0.35 μM), 10 (IC50 = 82.36 ± 1.93 μM), 11 (IC50 = 76.45 ± 0.13 μM), 16 (IC50 = 59.21 ± 1.00 μM), 18 (IC50 = 75.73 ± 1.54 μM), and 19 (IC50 = 76.43 ± 0.04 μM) exhibited moderate to weak anti-leishmanial potential, if compared with the standard pentamidine (IC50 = 5.09 ± 0.04 μM), whilst rest of the analogs were found to be inactive. [ABSTRACT FROM AUTHOR]- Published
- 2017
13. Comparative Antidiabetic Evaluation of Different Parts of Nicotiana Plumbajnifolia in Alloxan Induced Diabetic Mice.
- Author
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Ajaib, Muhammad, Fatima, Sameen, Kamran, Sairah Hafeez, Khan, Khalid Mohammed, Perveen, Shahnaz, and Shah, Shazia
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HYPOGLYCEMIC agents ,ALLOXAN diabetes ,MICE ,METFORMIN ,ALKALOIDS ,SAPONINS ,FLAVONOIDS ,TANNINS - Abstract
The present study was carried out to access the acute effects of methanolic extracts of various parts of Nicotiana plumbajnifolia in diabetic mice. Basic phytochemical evaluation showed the presence of alkaloids, saponins, flavonoids and tannins as the min compounds in the methanolic extract. Diabetes was induced experimentally in 12 hours fasted mice by intraperitoneally (i.p.) injecting alloxan (150 mg/kg). The methanolic extracts of Nicotiana plumbajnifolia stem, root, leaves and fruit were evaluated for antidiabetic potential in alloxan treated diabetic mice. The mice were categorized into six groups (n=5). The methanolic extracts of stems, leaves, root and fruit (250 mg/kg) were administered intraperitoneally once and changes in blood glucose levels were recorded at 6 and 24 hours. Metformin (2 g/kg) was administration intraperitoneally and used as positive control. Methanolic extracts of N. plumbajnifolia leaves showed maximum reduction in blood glucose level (95.33 ±13.6***) when compared with control diabetic group (280.2 ± 7.92). There was 26.6% decrease in blood glucose levels after 6 hours with metformin (2 g/kg) whereas leaves showed 46.3 % reduction. The stems, root and fruit showed 38.9, 39.3 and 42.9 % reduction in blood glucose six hours after dose administration. The leaves have maximum blood glucose reducing capacity. [ABSTRACT FROM AUTHOR]
- Published
- 2016
14. Anti-Cancer Potential of Benzophenone-Bis-Schiff bases on Human Pancreatic Cancer Cell Line.
- Author
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Khan, Khalid Mohammed, Rasheed, Huma, Fatima, Bibi, Hayat, Muhammad, Rahim, Fazal, Ullah, Hayat, Hameed, Abdul, Taha, Muhammad, Tahir, Affan, and Perveen, Shahnaz
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PANCREATIC cancer treatment , *ANTINEOPLASTIC agents , *BENZOPHENONES , *STRUCTURE-activity relationship in pharmacology , *CELL-mediated cytotoxicity , *SCHIFF bases - Abstract
Synthetic benzophenone-bis-Schiff bases (1-17) were evaluated for PC3 cell line inhibition. Most of the compounds showed cytotoxic effects but compounds 4, 8, 14, 16, and 17 were found to be potent. The growth inhibition of PC3 cells was in a concentration-dependent manner when treated with compounds 4, 8, 14, 16 and 17 (Figure-2) after 24 h exposure time. The IC50 values of all five most active compounds were calculated as 4 (IC50 = 24 ± 1.4 µM), 8 (IC50 = 29 ± 1.3 µM), 14 (IC50 = 66 ± 2.8 µM), 16 (IC50 = 28 ± 1.4 µM) and 17 (IC50 = 18 ± 2.8 µM) when compared with standard cisplatin (IC50 = 20 ± 1.1 µM). This study has identified potent anticancer agents. [ABSTRACT FROM AUTHOR]
- Published
- 2016
15. Amino Acid Linked Bromobenzoyl Thiourea Derivatives: Syntheses, Characterization and Antimicrobial Activities.
- Author
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Raheel, Ahmad, Imtiaz-ud-Din, Badshah, Amin, Rauf, Muhammad Khawar, Tahir, Muhammad Nawaz, Khan, Khalid Mohammed, Hameed, Abdul, and Andleeb, Sohaila
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THIOUREA ,CHEMICAL synthesis ,ANTI-infective agents ,THIOCYANATES ,NUCLEAR magnetic resonance spectroscopy ,DATA analysis - Abstract
Five new bromobenzoyl thiourea derivatives (1-5) linked with different amino acids were synthesized via the reaction of bromobenzoyl chloride with potassium thiocyanide and the corresponding amines. The synthetic compounds were characterized by single crystal XRD, IR and NMR (¹H
- and13 C- ) spectroscopy in addition to elemental analysis and melting point determinations. These compounds were also preliminary analyzed for antifungal and antibacterial activity against different strains of fungi and bacteria, respectively. The data suggest that the compounds exhibited promising antimicrobial activity and may prove potential lead compounds as antimicrobial agent. [ABSTRACT FROM AUTHOR]- Published
- 2016
16. A Facile Route towards the Synthesis of 2-(1H-indol-3-yl)-acetamides Using 1,1-Carbonyldiimidazole.
- Author
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Kanwal, Khan, Khalid Mohammed, Fatima, Bibi, Bano, Bilquees, and Salar, Uzma
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ACETAMIDE , *CHEMICAL synthesis , *IMIDAZOLES , *ACETIC acid , *ANILINE , *CHEMICAL yield - Abstract
A base-catalyzed one pot reaction has been developed for the synthesis of 2-(1H-indol-3-yl)- acetamides via coupling of 1,1-carbonyldiimidazole with 2-(1H-indol-3-yl) acetic acid resulting in the formation of a reactive intermediate which on treatment with different substituted anilines afford 2-(1Hindol- 3-yl)-acetamides in good yield. The use of base along with coupling reagent eases the formation of intermediate in minimum time. All the synthetic compounds were obtained in good to moderate yields, the use of various substituted anilines effects the yields of the products. Compounds 4-30 were synthesized and the structures of all the synthetic compounds were determined by using spectroscopic techniques such as ¹H-, 13C-NMR, EIMS and HRMS. [ABSTRACT FROM AUTHOR]
- Published
- 2016
17. Synthesis and Enzyme Inhibitory Studies of Some New N-Alkylated/Aralkylated N-(4-Ethoxyphenyl)-2,3-dihydrobenzo-[1,4]-dioxin-6-sulfonamides.
- Author
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Abbasi, Muhammad Athar, Islam, Mudassar, Aziz-Ur-Rehman, Siddiqui, Sabahat Zahra, Khan, Khalid Mohammed, Ashraf, Muhammad, and Asghar, Humna
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SULFONAMIDES ,CHEMICAL synthesis ,ENZYME inhibitors ,AQUEOUS solutions ,LITHIUM hydride - Abstract
The research endeavor was aimed to synthesize N-alkyl/aralkylated-N-(4-ethoxyphenyl)- 2,3-dihydrobenzo-[1,4]-dioxine-6-sulfonamides and to evaluate their enzyme inhibitory potential. The target molecules were synthesized in two steps. The first step involved the reaction of 4- ethoxyaniline (1) with N-2,3-dihydrobenzo[1,4]-dioxin-6-sulfonyl chloride (2) under dynamic pH control maintained by 10% aqueous Na
2 CO3 to yield N-(4-ethoxyphenyl)-2,3-dihydrobenzo-[1,4]- dioxine-6-sulfonamide (3). In second step parent compound 3 was reacted with various alkyl/aralkyl halides (4a-l) in N,N'-dimethylformamide and catalytic amount of lithium hydride to accomplish some new N-alkyl/aralkylated-N-(4-ethoxyphenyl)-2,3-dihydrobenzo-[1,4]-dioxine-6-sulfonamides (5a-l). Probable structures of the synthesized compounds were characterized by contemporary spectral techniques i.e. IR, ¹H-NMR and EIMS and were finally evaluated for enzyme inhibitory potential against a-glucosidase and urease. The synthesized compounds exhibited moderate to weak therapeutic potential throughout the series. [ABSTRACT FROM AUTHOR]- Published
- 2016
18. Investigation of the Chemical Composition of the n-Hexane Fraction of the Spirogyra.
- Author
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Hussain, Zahid, Khan, Khalid Mohammed, Hayat, Ghazanfar, Zaman, Khair, Karim, Aneela, Perveen, Shahnaz, and Haider, Syed Moazzam
- Subjects
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SPIROGYRA , *HEXANE , *FRACTIONS , *BIOMASS energy , *EXTRACTION (Chemistry) , *CHEMISTRY experiments , *GAS chromatography/Mass spectrometry (GC-MS) , *CHROMATOGRAMS - Abstract
In view of the importance of algae as biomass for the resource recovery the non-polar fraction of the Sopirogyra was analyzed. This fraction was obtained both by hot and cold extraction process in separate experiments using n-hexane as solvent. The qualitative and quantitative analysis of the extract was carried out using GC-MS and GC equipped with FID in separate experiments. The nature of products was confirmed using total ion chromatograms as well as fragmentation pattern. The concentration of the major compounds was determined using the peak area. This fraction of Spirogyra was found to have 51.19 % of various types of alcohols, 47.64% of various amines and small quantities of thiol and ketones in addition to small quantities of two unknown compounds. The possible uses of this extract as resource is also discussed in this communication. [ABSTRACT FROM AUTHOR]
- Published
- 2016
19. Phytochemical, Antimicrobial and Antioxidant Screening of Fruits, Bark and leaves of Lagerstroemia indica.
- Author
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Ajaib, Muhammad, Arooj, Taha, Khan, Khalid Mohammed, Farid, Sidra, Ishtiaq, Muhammad, Perveen, Shahnaz, and Shah, Shazia
- Subjects
COMMON crape myrtle ,ANTI-infective agents ,ANTIOXIDANTS ,PHYTOCHEMICALS ,ANTHRAQUINONES ,MICROBIOLOGY ,PLANTS - Abstract
The present study was conducted to evaluate phytochemicals, antimicrobial and antioxidant potential of Lagerstroemia indica L. The phytochemical screening of L. indica revealed the presence of active metabolites such as anthraquinones, reducing sugars, terpenoids, flavonoids, saponins, tannins, alkaloids and cardiac glycosides. Antimicrobial assessment was carried out against Gram-positive bacteria (Bacillus subtilis, Staphylococcus aureus), Gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli) and fungal strains (Aspergillus oryzae and Aspergillus niger). Maximum antibacterial potential (58.33 ± 0.88 mm) was exhibited by petroleum ether extract of bark against B. subtilis. The maximum antifungal potential 40.33 ± 0.88 mm and 40.0 ± 1.15 mm against A. niger was observed by chloroform extract of bark and fruits respectively. The antioxidant potential was assessed using five assays viz. ABTS activity, DPPH° radical scavenging activity, metal chelating activity, total flavonoid contents and total phenolic contents. Highest TEAC value 7.946 ± 0.04 mM trolox for ABTS+ assay was observed by aquous extract of leaves. The highest values for total flavonoid contents 1185.740 ± 0.01 µg/ml and total phenolic contents 40.333 ± 0.23 µg/ml was exhibited by petroleum ether bark extract. The maximum metal chelating activity 60.302 ± 0.93 was observed by petroleum ether extract of fruit. The highest value of % DPPH° (92.92 ± 0.08 %) was observed by aquous extract of bark. [ABSTRACT FROM AUTHOR]
- Published
- 2016
20. Sonic and Microwaves Assisted Redox Reactions of the Hydrolysates of Protein for the Preparation of Rechargeable Battery.
- Author
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Hussain, Zahid, Khatak, Karishma, Sardar, Anila, Khan, Khalid Mohammed, and Perveen, Shahnaz
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OXIDATION-reduction reaction ,HYDROLYSIS ,STORAGE batteries ,CHEMICAL sample preparation ,SOLUTION (Chemistry) - Abstract
Long recharging time is one of the serious limitations of batteries. One of the best solutions for quick redox reactions via the use of microwave and sound-assisted reversible redox reaction is presented in this work. A wireless charged prototype battery based on the redox reactions of hydrolyzed waste protein was designed. The effect of experimental conditions like time of charging, nature of media and strength of the acid on the voltage of this prototype battery was investigated. The experimental data was explained on the basis of the previous work on protein peptides and amino acids by various workers. [ABSTRACT FROM AUTHOR]
- Published
- 2016
21. 5-Nitroimidazole Derivatives and their Antimicrobial Activity.
- Author
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Khan, Khalid Mohammed, Salar, Uzma, Tauseef, Saima, Miana, Ghulam Abbas, Yousuf, Sahar, Naz, Farzana, Taha, Muhammad, Khan, Saifullah, and Perveen, Shahnaz
- Subjects
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NITROIMIDAZOLES , *ANTI-infective agents , *ASPERGILLUS flavus , *CORYNEBACTERIUM diphtheriae , *SUBSTITUENTS (Chemistry) , *ANTIFUNGAL agents - Abstract
5-Nitroimidazole derivatives 2-8 were synthesized from secnidazole. The syntheses were accomplished in two steps which start from the oxidation of secnidazole to the secnidazolone 1. Secnidazolone 1 was converted into its hydrazone derivative 2-8 by treating with different substituted acid hydrazide. Compounds 2-8 were evaluated for their antimicrobial activity against Gram-positive and Gram-negative bacteria, compounds 3 and 4 showed the significant activity against Staphylococcus epidermidis, however, compound 2 showed good inhibitions against Corynebacterium diphtheria when compared with the standard. Compound 3 showed good inhibitory potential against tested Gram-negative bacterial strains i.e. Enterobacter aerogene, Escherichia coli, Salmonella typhi, Salmonella paratyphi A, Shigella flexeneri and Vibrio choleriae. All synthetic derivatives were also tested against eight fungal stains, however, they were weekly active against Aspergillus flavus and Candida albican. The synthesized compounds were characterized by different spectroscopy techniques. [ABSTRACT FROM AUTHOR]
- Published
- 2016
22. In Vitro Antileishmanial Activities of 2-Aryl-4(3H)-quinazolinones.
- Author
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Perveen, Shama, Saad, Syed Muhammad, Perveen, Shahnaz, Hameed, Abdul, Alam, Muhammad Tanveer, Khan, Khalid Mohammed, and Choudhary, M. Iqbal
- Subjects
QUINAZOLINONES ,DRUG development ,LEISHMANIA ,STRUCTURE-activity relationship in pharmacology ,PENTAMIDINE ,THERAPEUTICS - Abstract
A series of synthetic 2-aryl-4(3H)-quinazolinones (1-25) was evaluated for in vitro antileishmanial activities against promastigotes of Leishmania major. Compound 1, with nitro group installed at C-4', was found to be the most active analog having the IC
50 value of 35.8 ± 0.1 µM against the standard, pentamidine (IC50 = 5.09 ± 0.09 µM). Fourteen other derivatives i.e. 2, 5-8, 10- 12, 14, 16, 19, 22, 24, ad 25, showed a moderate to weak antilieshmanial activity with IC50 values between 62.8 - 90.45 µM. The results indicate the potential of these compounds as leads for further studies towards the development of antileishmanial drugs. [ABSTRACT FROM AUTHOR]- Published
- 2016
23. Synthesis, Characterization and Antimicrobial Evaluation of some Thiazole-Derived Carbamates, Semicarbazones, Amides and Carboxamide.
- Author
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El-Sayed, Nahed Nasser E., AL-Balawi, Nawal Ali, Alafeefy, Ahmed M., AL-ALShaikh, Monirah A., and Khan, Khalid Mohammed
- Subjects
CARBAMATES synthesis ,ANTI-infective agents ,SEMICARBAZONES ,CARBOXAMIDES ,AMIDE synthesis ,NUCLEOPHILIC substitution reactions - Abstract
This study comprises the synthesis and characterization of twenty thiazole-derived carbamates (3a-e), N-substituted amides (8a-h) and carboxamide (10) from 2-aminothiazoles (1a, b) via nucleophilic substitution reactions with activated carbonyl compounds including, chloroformates (2a-d), acid chlorides (7a-e) and glutaric anhydride (9), respectively. Sequential hydrazinolysis of carbamate (3e) and condensation with a variety of aldehydes and ketones (5a-d) afforded the corresponding semicarbazones (6a-d). Some selected synthesized compounds were subjected to in vitro antimicrobial evaluation against common pathogens including, Gram+ve bacteria Bacillus subtilis (NRRL B-543) and Staphylococcus aureus, Gram-ve bacteria Escherichia coli (NRRLB-21), yeasts-Candida albicans (NRRLY-477) and Saccharomyces cercvisiae (NRRL Y-567) and fungs Asperigillus niger (NRRL 599). Screening results revealed that most of the tested compounds possess good antimicrobial activity compared to standard drugs. The highest inhibitory effects against Gram-ve Escherichia coli, Gram+ve Staphylococcus aureus, yeast Candida albicans and fungus Aspergillus niger was displayed by amide (8g) bearing the thiophene moiety. [ABSTRACT FROM AUTHOR]
- Published
- 2016
24. Phytochemical Screening, Antimicrobial and Antioxidant Activities of Ficus natalensis.
- Author
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Ajaib, Muhammad, Almas, Muniza, Khan, Khalid Mohammed, Perveen, Shahnaz, and Shah, Shazia
- Subjects
PHYTOCHEMICALS ,FICUS (Plants) ,ANTIBACTERIAL agents ,THERAPEUTIC use of plant extracts ,ANTI-infective agents ,ANTIOXIDANT testing - Abstract
Phytochemical screening, antimicrobial and antioxidant potential of the bark and leaves extracts of Ficus natalensis were carried out by using various techniques. Phytochemical analysis showed the presence of terpenoids, alkaloids, flavonoids, tannins, saponins, cardiac glycosides and reducing sugars in different extracts of Ficus natalensis. The antibacterial potential against S. aureus was reported as most promising amongst all. The petroleum ether extract of leaves with a zone of inhibition 50 ± 0.51 mm and bark extracts with a zone of inhibition 55.7 ± 1.15 mm inhibited S. aureus. The chloroform leaves extract also showed an inhibition zone of 50 ± 2 mm against S. aureus. The antifungal potential of methanol bark extract at 43.7 ± 1.527 mm and petroleum ether extracts of bark with zones of inhibition 37 ± 0.577 mm against A. niger showed most prominent activity. By using different assays, the extracts were screened for the antioxidant potential. The estimation of antioxidant activity by metal chelating activity revealed that water extract of leaves was most active with a value of 74.673 ± 0.302 percentage bound iron. The chloroform extract of bark showed highest flavonoid content (1005.53 ± 0.503 mg/mL of quercetin), whereas chloroform extract of leaves exhibited maximum phenolic content (21.626 ± 0.545 mg/g of GAE). In ABTS assay, water extract of leaves showed maximum TEAC value (7.713 ± 0.7 mM of trolox equivalent). The highest free radical scavenging DPPH percentage was observed with distilled water extract of bark (91.92 ± 0.08%). [ABSTRACT FROM AUTHOR]
- Published
- 2016
25. Forced Degradation Studies of Antipsychotic Iloperidone by UV Spectrophotometry.
- Author
-
Karim, Zahida, Karim, Aneela, Khan, Khalid Mohammed, Shafi, Nighat, and Saeed, Danya Roohi
- Subjects
ANTIPSYCHOTIC agents ,ULTRAVIOLET spectrophotometry ,DRUG development ,PHOTOLYSIS (Chemistry) ,HYDROLYSIS - Abstract
A simple, rapid and cost-effective forced degradation study of Iloperidone was conducted by UV spectrophotometric method. Complete validation was performed for linearity, accuracy, and precision at the concentration range of 10-70 µg mL
-1 . Iloperidone was subjected to different stress conditions recommended by International Conference on Harmonization (ICH). The drug has been found susceptible to acidic and alkaline hydrolysis. However, no dry heat or photolytic degradation was observed. The results of the study can facilitate the stability indicating method development, selection of storage conditions and better understanding of the intrinsic stability characteristics of the drug molecule. [ABSTRACT FROM AUTHOR]- Published
- 2016
26. An Efficient Microwave Assisted Synthesis of Triphenodioxazines Using Chloranil as Oxidizing Agent.
- Author
-
Ullah, Muhammad Najeeb, Munawar, Munawar Ali, Knight, David William, Khan, Misbahul Ain, Waheed, Amran, and Khan, Khalid Mohammed
- Subjects
OXAZINES ,HETEROCYCLIC compounds synthesis ,MICROWAVE chemistry ,CHLORANIL ,POTASSIUM compounds ,OXIDIZING agents - Abstract
An efficient new method for the preparation of triphenodioxazines (TPDOs) using pchloranil as oxidizing agent in conc. H2SO4 under microwave irradiation at 120oC is reported. This method is more efficient than the previously described microwave method using potassium persulfate as oxidising agent in conc. H2SO4 as it provides the cyclized product within 8-10 minutes with comparatively higher yields. [ABSTRACT FROM AUTHOR]
- Published
- 2016
27. Comparative Anti-Diabetic Evaluation of Different Parts of Himalrandia tetrasperma in Alloxan Induced Diabetic in Mice.
- Author
-
Ajaib, Muhammad, Latif, Misbah, Kamran, Sairah Hafeez, Khan, Khalid Mohammed, Perveen, Shahnaz, Shah, Shazia, and Kareen, Aneela
- Subjects
HYPOGLYCEMIC agents ,ALLOXAN diabetes ,ANIMAL models of diabetes ,METFORMIN ,BLOOD sugar measurement ,COMPARATIVE studies - Abstract
The present experiments were designed to investigate the acute effects of methanolic extracts of various parts of H. tetrasperma in diabetic mice. The basic phyto-chemical study showed the occurrence of alkaloids, saponins, flavonoids and tannins as main phyto-constituents in the methanolic extract. Diabetes was induced experimentally in mice by intra peritoneally injecting alloxan (150 mg/kg i.p.). In acute study, methanolic H. tetrasperma extracts of various parts of plant were evaluated for anti-diabetic potential in alloxan induced diabetic mice. Extracts of leaves, bark and seeds (250 mg/kg, i.p) and metformin (250 mg/kg i.p) were given intra peritoneal in alloxan treated diabetic mice and blood glucose levels were measured at 0, 360 and 24 h. There was significant lowering of blood glucose level at 1 h after treatment, in diabetic mice treated with methanolic extracts of bark (182.3 ± 3.6 mg/dL), leaves (178.5 ± 1.2 mg/dL) and seeds (156.3 ± 11.3 mg/dL) when compared with control diabetic group (280 ± 7.92 mg/dL). Highly significant results were also obtained at 24 h after treatment with methanolic extracts of bark (187.67 ± 1.2 mg/dL), leaves (170.66 ± 2.3 mg/dL) and seeds (142 ± 8.7 mg/dL) when compared with control diabetic group (257.7 ± 6.7 mg/dL). It is concluded that methanolic extract of all parts possess significant anti-diabetic activity which is due to the presence of phytochemicals, i.e. alkaloids, flavonoids, phenols, saponins, tannins and it can be further evaluated for the mechanism involved. [ABSTRACT FROM AUTHOR]
- Published
- 2016
28. Synthesis, Characterization, Antimicrobial and Antileishmanial Activities of Amide derivatives of L-tartaric acid.
- Author
-
Sher Wali Khan, Zaidi, Javid H., Nasser, Nahed, El-Sayed, E., Khan, Khalid Mohammed, Yousuf, Sammer, Khan, Momin, Nadhman, Akhtar, Naveed Umar, M., Perveen, Shahnaz, and Miana, Ghulam Abbas
- Subjects
TARTARIC acid ,AMIDE synthesis ,ANTI-infective agents ,X-ray crystallography ,PROMASTIGOTE - Abstract
Sixteen (16) chiral, amides were synthesized from commercially available L-tartaric acid, having two asymmetric centers and C2 axis of symmetry. The diacid functionality of L-tartaric acid was protected as dimethyl ester and dihydroxy groups as acetonoid. The partial hydrolysis of acetonoid of dimethyl ester gave the corresponding monoester. Monoester upon treatment with different substituted aromatic amines gave desired amides (1-8). Amides (1-8) afforded deprotected compounds (9-16) after reacting with acetyl chloride and methanol. All the compounds were characterized by using spectroscopic techniques such as IR,
1 H-NMR,13 C-NMR, and EIMS. The compounds gave reasonable elemental analyses. The structure of compound 6 was unambiguously obtained by X-ray crystallography. Protected (1-8) and deprotected amides (9-16) were tested for their antileishmanial (against Leshmania tropica KWH23 Promastigotes) and antimicrobial activities at different concentrations against different strains of bacteria and fungi. [ABSTRACT FROM AUTHOR]- Published
- 2016
29. Syntheses and Application of Sulfonic Acid Dyes on Wool Fabric.
- Author
-
Akhtar, Zeeshan, Farooq, Muhammad, Kazimi, Mohib Raza, Parveen, Rasheeda, Ali, Syed Ishrat, Karim, Aneela, and Khan, Khalid Mohammed
- Subjects
SULFONIC acids ,ACID dyeing (Textiles) ,SPECTROPHOTOMETERS ,WOOL textiles ,MASS spectrometry ,AMINE derivatives - Abstract
Syntheses of acid dyes were done by reacting diazotized substituted aryl amines and substituted naphthalene sulfonic acids as coupling component. Structure elucidation of these synthetic dyes was carried out by their UV-visible, IR, 1HNMR spectra, elemental analysis and negative MALDI-TOF mass spectrometric analysis. The aim of this research is the application of synthesized acid dyes on wool fabric and fastness properties by light, washing, perspiration, crocking data from color spectrophotometer studied. [ABSTRACT FROM AUTHOR]
- Published
- 2016
30. Synthesis, Characterization and Biological Evaluation of N'-Substituted-2-(5-(4- substitutedphenyl)-1,3,4-Oxadiazol-2-ylthio)acetohydrazide Derivatives.
- Author
-
Rasool, Shahid, Aziz-ur-Rehman, Abbasi, Muhammad Athar, Siddiqui, Sabahat Zahra, Ahmad, Irshad, Malik, Rabia, and Khan, Khalid Mohammed
- Subjects
OXADIAZOLES ,CARBOXYLIC acids ,ANTIBACTERIAL agents ,LIPOXYGENASES ,ENZYMES - Abstract
Hydrazone derivatives bearing heterocyclic moiety have been synthesized to evaluate their antibacterial and enzyme inhibition activity. Two p-substituted carboxylic acids (1a and 1b) have been utilized to synthesize ethyl esters (2a and 2b), carbohydrazides (3a and 3b), 5- substituted-1,3,4-oxadiazol-2-thiols (4a and 4b), heterocyclic ethyl esters (5a and 5b) and finally acetohydrazides (6a and 6b). The final hydrazone derivatives, 8a-j and 9a-j, were synthesized by the reaction of 6a and 6b with different un/mono substituted benzaldehydes (7a-j) in methanol. The synthesized compounds were characterized by spectral data of IR,
1 H-NMR and EIMS. The evaluation of these molecules for their antibacterial and lipoxygenase inhibition activities rendered 8g suitable antibacterial agent and lipoxygenase inhibitor and the remaining ones as moderate inhibitors. [ABSTRACT FROM AUTHOR]- Published
- 2016
31. 1-(2,4-Dihydroxyphenyl)-1-ethanone Hydrazone Derivatives as Notable Butyrylcholinesterase Inhibitors.
- Author
-
Abbasi, Muhammad Athar, Niazi, Sikander Khan, Aziz-Ur-Rehman, Siddiqui, Sabahat Zahra, Hussain, Ghulam, Rasool, Shahid, Ashraf, Muhammad, Rahman, Jamil, and Khan, Khalid Mohammed
- Subjects
BUTYRYLCHOLINESTERASE ,SCHIFF bases ,HYDROXYACETOPHENONES ,CHEMISTRY education ,HYDRAZINE - Abstract
Azomethine group of Schiff bases is known to express valuable biological activities. 1- (2,4-Dihydroxyphenyl)-1-ethanone N'-substituted hydrazone derivatives, 4a-s, were synthesized in multistep. The starting material 2,4-dihydroxyacetophenone (1) was stirred with hydrated hydrazine to yield 1-(2,4-dihydroxyphenyl)-1-ethanone hydrazone (2) which was further reacted with (un)substituted benzaldehydes, 3a-s, to acquire the target molecules, 4a-s. Moreover, the synthesized derivatives 4a-s was characterized via IR, EI-MS,
1 H-NMR and13 C-NMR spectral techniques. Most of the compounds were found to be valuable inhibitors of butyrylcholinesterase enzyme. [ABSTRACT FROM AUTHOR]- Published
- 2016
32. Nicotiana plumbaginifolia: A Rich Antimicrobial and Antioxidant Source.
- Author
-
Ajaib, Muhammad, Fatima, Sameen, Khan, Khalid Mohammed, Perveen, Shahnaz, and Shah, Shazia
- Subjects
NICOTIANA plumbaginifolia ,ANTI-infective agents ,ANTIOXIDANTS ,CHLOROFORM ,METHANOL ,CHEMICAL synthesis ,ESCHERICHIA coli ,THERAPEUTICS - Abstract
Antimicrobial and antioxidant activities of plant Nicotiana plumbaginifolia Viv. Were carried out using various techniques. The petroleum ether, chloroform, methanol and aqueous extracts of the N. plumbaginifolia were obtained by maceration technique. The maximum antibacterial potential was exhibited by chloroform leaves extract (76.3 ± 0.3 mm), methanolic root extract (69 ± 0.8 mm) and petroleum ether root extract (67 ± 1.7 mm) against P. aureginosa. Methanolic root extract possessed 64 ± 2.3 mm zone of inhibition against E. coli, whereas chloroform root extract displayed 49 ± 0.8 mm against B. subtilis. Chloroform root extract showed 48 ±1.2 against S. aureus. The maximum zone of inhibition of antifungal potential was displayed by methanolic extracts of leaves against A. niger (43 ± 0.8 mm) and F. solani (43 ± 1.6 mm). The MIC assay was determine for further analysis which showed the MIC value of methanolic root extract (0.04 ± 0.1 mg/mL) against E. coli and the MIC value was noticed (0.108 ± 0.04 mg/mL) against A. niger by methanolic root extract. Antioxidant potential was determined using four methods i.e. [1,1- diphenyl-2-picrylhydrazyl radical (DPPH) scavenging activity, total antioxidant activity (TAA), total phenolic contents (TPC) and metal chelating activity. The highest value of % DPPH was observed 90.56 at 1000 μl concentration in petroleum ether extract. The maximum values of TAA, TPC, FRAP and FTC were 1.352 ± 0.01, 1.683 ± 0.09 and 80.66 ± 0.08, respectively. [ABSTRACT FROM AUTHOR]
- Published
- 2016
33. Enzyme Inhibitory and Molecular Docking Studies on Some Organic Molecules of Natural Occurrence.
- Author
-
Abbasi, Muhammad Athar, Hussain, Ghulam, Aziz-ur-Rehman, Shahwar, Durre, Khan, Khalid Mohammed, Mohyuddin, Ayesha, Ashraf, Muhammad, Rahman, Jameel, Lodhi, Muhammad Arif, and Khan, Farman Ali
- Subjects
ENZYME inhibitors ,XANTHINE oxidase ,LIPOXYGENASES regulation ,CINCHONIDINE ,MOLECULAR physics ,INTERMOLECULAR forces ,REACTIVE oxygen species - Abstract
In the present study, in vitro enzyme inhibitory studies on cinchonidine (1), cinchonine (2), quinine (3), noscapine (narcotine, 4) and santonine (5) were carried out. The various enzymes included in the study were lipoxygenase, xanthine oxidase, acetyl cholinesterase, butyryl cholinesterase and protease. The results revealed that 2, 3, and 4 were moderate active against lipoxygenase and xanthine oxidase enzymes. The molecule 3 possessed weak activity against butyryl cholinesterase enzyme while remaining molecules were inactive against this enzyme. However, all these compounds were inactive against acetyl cholinestrase and protease enzymes. The synthesized compounds were computationally docked into the active site of lipoxygenase enzyme. The compounds 3 and 4 showed decent interactions, hence strengthening the observed results. [ABSTRACT FROM AUTHOR]
- Published
- 2016
34. Biology-Oriented Syntheses (BIOS) of Novel Santonic-1,3,4-oxadiazole Derivatives under Microwave-Irradiation and their Antimicrobial Activity.
- Author
-
Salar, Uzma, Miana, Ghulam Abbas, Khan, Khalid Mohammed, Naz, Farzana, Siddiqui, Nida Iqbal, Taha, Muhammad, Tauseef, Saima, Khan, Saifullah, and Perveen, Shahnaz
- Subjects
OXADIAZOLES ,CHEMICAL derivatives ,ANTI-infective agents ,SANTONIC acid ,STAPHYLOCOCCUS epidermidis - Abstract
Novel 2-thio substituted 1,3,4-oxadiazole derivatives of santonic acid (13-18) were synthesized. The synthesis of these derivatives was comprised of six steps which start from the basic hydrolysis of α-santonin 1 to the santoninic acid 2 followed by in situ rearrangement of 2 into santonic acid 3. Santonic acid 3 was then converted into its acyl imidazole derivative 4 followed by hydrazinolysis to give santonic carbohydrazide 5 which was further converted into santonic-1,3,4-oxadiazole-2-thiol 6. Santonic-1,3,4-oxadiazole-2-thiol 6 was alkylated to afford 2-thio substituted 1,3,4-oxadiazole derivatives of santonic acid (13-18). All the synthetic steps were carried out under microwave irradiation in controlled parameters. Compounds 13-18 along with intervening intermediates 5 and 6 were evaluated for their antimicrobial potential. Compound 14 showed appreciably good activity against Staphylococcus epidermidis. On the other hand compounds 6 and 17 demonstrated good activity against Escherichia coli and Shigella flexeneri, respectively. Compound 6 showed good antifungal activity. The synthesized compounds were characterized by different spectroscopy techniques. [ABSTRACT FROM AUTHOR]
- Published
- 2015
35. Synthesis, Antimicrobial, Antioxidant and Nematicidal Activity of (2E,4E)-5-(Benzo[d] [1,3]dioxol-5yl)penta-2,4-dienamides.
- Author
-
Wahab, Aneela, Sultana, Amina, Khan, Khalid Mohammed, Sherwani, Sikandar K., Perveen, Zeba, and Karim, Aneela
- Subjects
AMIDE synthesis ,NEMATOCIDES ,SOUTHERN root-knot nematode ,VITAMIN C ,CARBON dioxide - Abstract
The amides of piperic acid have been synthesized via the condensation of piperic acid with amines. The structural characterization was done by IR,
1 H-NMR, EI-MS and elemental analysis. The amides 3a-3o were evaluated for their biological activity. It has been found that among others the newly synthesized compound 3f, 3k, 3m, and 3o have great potential against root-knot nematode Meloidogyne incognita that usually affect tomato crop. These compounds exhibited 92, 96, 82 and 95% mortality rate at lethal concentration (LC50 ) 4.4, 3.4, 4.5 and 3.5 mg/mL, respectively. Conventionally used nematicide furadan was taken as standard. Compound 3h, 3c and, 3j exhibited significant anti-oxidant activities against 1,1-diphenylpicrylhydrazil (DPPH) radical with 80, 70 and 72% inhibition (EC50 = 625, 937 and 937.5 µg/mL), respectively. Ascorbic acid was used as standard. When tested for antimicrobial activity 3m was found to be the most active one showing zone of inhibition in the range of 18-30 mm against all tested microbial strains. Good biological activities of synthetic amides indicate their ability to behave as a good antimicrobial and nematicidal agent. [ABSTRACT FROM AUTHOR]- Published
- 2015
36. Antileshmanial Activities of Synthetic Substituted 2-phenyl-4-[phenylmethylidene]-1,3-oxazol-5(4H)-ones.
- Author
-
Khan, Saadia Razi, Ghouri, Nida, Karim, Aneela, Naz, Farzana, Fakhri, Muhammad Imran, Perveen, Shahnaz, Khan, Khalid Mohammed, and Choudhary, Muhammad Iqbal
- Subjects
OXAZOLES ,PENTAMIDINE ,LEISHMANIASIS treatment ,LEISHMANIA ,AMINO acid synthesis - Abstract
Substituted 2-phenyl-4-[phenylmethylidene]-1,3-oxazol-5(4H)-ones 1-27 were evaluated for their activity against Leishmania major. Compounds 1-27 demonstrated in vitro antileishmanial activities with IC
50 values between 28.9 - 69.05 μM, as compared to standard drug pentamidine (IC50 = 5.09 ± 0.04 μM). Compounds 12 (IC50 = 28.90 ± 1.10 μM), 24 (IC50 = 31.4 ± 2.15 μM), 13 (IC50 = 35.0 ± 3.18 μM), 16 (IC50 = 35.0 ± 3.13 μM), and 25 (IC50 = 35.0 ± 3.18μM) displayed signifiant antileishmanial activities. Whereas, compounds 8-10, 15, 19, and 26 with IC50 values of 62.2 ± 3.36, 57.8 ± 2.30, 57.72 ± 5.02, 56.18 ± 4.40, 57.85 ± 2.25, 69.05 ± 6.20, 54.8 ± 1.50, and 57.8 ± 2.30 μM showed a moderate antileishmanial activities. [ABSTRACT FROM AUTHOR]- Published
- 2015
37. Synthesis of 4-Amino-1,5-dimethyl-2-phenylpyrazolone Derivatives and their Antioxidant Activity.
- Author
-
Khan, Khalid Mohammed, Khan, Akbar, Taha, Muhammad, Salar, Uzma, Hameed, Abdul, Ismail, Nor Hadiani, Jamil, Waqas, Saad, Syed Mohammed, Perveen, Shahnaz, and Kashif, Syed Muhammad
- Subjects
- *
CHEMICAL synthesis , *ETHANES , *SCHIFF bases , *ANTIOXIDANTS , *HYDROXYL group - Abstract
Schiff bases of 4-amino-1,5-dimethyl-2-phenylpyrazolone (2-18) were synthesized by treating with different benzaldehyde derivatives and tested for in vitro antioxidant activity. Synthesized Schiff base derivatives (2-18) were characterized by various spectroscopic techniques. Compounds specially having hydroxyl substituents showed good DPPH radical scavenging activity having IC50 values between 15.16 and 48.26 µM. Compounds 3-7 showed stronger potency than the standard (n-propyl gallate, IC50 = 30.27 ± 0.25 µM). However, in the superoxide anion radical assay, derivatives 2, 4, 5, 6 and 7 showed better potency than the standard (n-propyl gallate, IC50 = 106.34 ± 1.60 µM). [ABSTRACT FROM AUTHOR]
- Published
- 2015
38. Preparation of a Rechargeable Battery Using Waste Protein from the Fish Scales.
- Author
-
Hussain, Zahid, Bashir, Nadia, Ahmad, Owais, Khan, Khalid Mohammed, Karim, Aneela, Perveen, Shahnaz, Khan, Momin, and Rafiq, Nasim
- Subjects
STORAGE batteries ,OXYTOCIN ,COLLAGEN ,OXIDATION ,ELECTRIC equipment - Abstract
The electrochemical redox reactions of the oxytocin and fish scale protein which are mainly collagen were exploited for the preparation of a rechargeable protein battery named as fish scale battery. This battery was found to depend upon the concentration of oxidizing and reducing agents, voltage of the charger and the time for charging. Some of these parameters were optimized using a single cell of this battery and some others were optimized by using five cell battery. The five cell protein battery gives a maximum and stable voltage of 8500 millivolt. The way of charging and theoretical aspects of the battery is also discussed in this communication. [ABSTRACT FROM AUTHOR]
- Published
- 2015
39. Appraisal of β-Phellandrene in Callus Cultures of Momordica charantia L. Cultivars, Jaunpuri and Jhalri.
- Author
-
Ali, Safdar, Tariq, Alveena, Ajaib, Muhammad, Khan, Khalid Mohammed, Perveen, Shahnaz, and Shah, Shazia
- Subjects
PLANT reproduction ,MOMORDICA charantia ,CULTIVARS ,GERMINATION ,MOMORDICA - Abstract
Secondary metabolite β-phellandrene was analyze in callus cultures of two varieties of Momordica charantia L. i.e. Jaunpuri and Jhalri. Conditions for seed germination and callus induction were optimized. Seedlings grown under aseptic conditions served as explant sources. 6- Benzylaminopurine (BAP) and 2,4-dichlorophenoxyacetic acid (2,4-D) supplemented in Murashige and Skoog's (MS) medium were scrutinized as the most suitable combination of plant growth regulators with different concentrations for callus induction in both the varieties. Cotyledon explant of (cultivars) cv. Jaunpuri revealed maximum callus induction with 1.0 mgl
-1 BAP and 1.5 mgl-1 2,4- D in eight days as compared to internode, apical bud and leaf. Cotyledon and leaf explants of cv. Jhalri responded to 1.5 mgl-1 BAP and 1.0 mgl-1 2,4-D in nine days for callus and internode and apical bud with 1.0 mgl-1 BAP and 1.5 mgl-1 2,4-D. Best grown calli from different explants were analyzed through GC-MS for production of secondary metabolites. Along with other secondary metabolites β-phellandrene was the most prominent secondary metabolites found in in vitro grown callus cultures of both the varieties. The callus cultures of cv. Jaunpuri produced substantial amount of β-phellandrene i.e. up to 30 percent of the total secondary metabolites as compared to calli from cv. Jhalri explants. The callus cultures of M. charantia can prove the best alternative, rapid and uninterrupted source for natural β-phellandrene production. [ABSTRACT FROM AUTHOR]- Published
- 2015
40. Casearia Tomentosa: A Potential Antimicrobial and Antioxidant Source.
- Author
-
Ajaib, Muhammad, Khalid, Shazia, Khan, Khalid Mohammed, Siddiqui, Sabahat Zahra, Abbasi, Muhammad Athar, Perveen, Shahnaz, and Shah, Shazia
- Subjects
CASEARIA ,ANTIOXIDANTS ,HYDROXYL group ,ANTI-infective agents ,CHEMICAL reactions - Abstract
The present work is an effort to discover anti-microbial and antioxidant potential of bark and leaf extracts of Casearia tomentosa Roxb. The extracts provide excellent to satisfactory antimicrobial results with maximum antibacterial potential 37 ± 3.03 mm exhibited by methanolic leaf extract against E. coli by agar-well diffusion assay and 0.013 ± 0.05 (at 0.9 mg/L) in opposition to B. subtilis by broth-dilution (MIC) analysis. Methanolic leaf extract also produces significant antifungal result against F. solani with value of 34.5 ± 4.59 mm and against A. oryzae with MIC value of 0.010 ± 0.001 (at 0.9 mg/L). Various extracts showed significant DPPH activity with bark petroleum-ether extract displaying 92.5 ± 0.03% radical scavenging potential and chloroform extract of leaf exposing IC
50 : 10.77 ± 1.02 µg/mL. The antioxidant potential of the plant is further verified by employing TAA (maximum at 1.131 ± 0.10 by bark methanolic extract), FRAP (highest at 296 ± 0.23 by chloroform bark extraction) and TPC (peak at 86.16 ± 0.08 GAE mg/mL of chloroform bark extract). [ABSTRACT FROM AUTHOR]- Published
- 2015
41. 2-(2'-Pyridyl) Benzimidazole Analogs and their β-Glucuronidase Inhibitory Activity.
- Author
-
Kamil, Arfa, Akhtar, Shamim, Noureen, Shagufta, Saify, Zafar Saied, Jahan, Sarwat, Khan, Khalid Mohammed, Rahim, Fazal, Mushtaq, Nousheen, Arif, Muhammad, Perveen, Shahnaz, and Chaudhary, Muhammad Iqbal
- Subjects
BENZIMIDAZOLES ,CHEMICAL synthesis ,CHEMICAL reactions ,GLUCURONIDASE ,GLYCOSIDASES - Abstract
Synthesis of 2-(2'-pyridyl) benzimidazole analogs 1-11 have been carried out and evaluated for in vitro β-glucuronidase inhibitory potential. The compounds 4 (IC
50 = 4.06 ± 0.34 µM), 5 (IC50 = 09.63 ± 0.81 µM), 1 (IC50 = 19.66 ± 0.44 µM), 7 (IC50 = 24.75 ± 0.25 µM), 6 (IC50 = 26.30 ± 1.37 µM), and 3 (IC50 = 32.11 ± 0.89 µM), showed β-glucuronidase inhibitory activity superior to the standard D-saccharic acid 1,4-lactone, with (IC50 = 48.4 ± 1.25 µM). Based on structure-activity relationship, we discover a new class of potent β-glucuronidase inhibitors. [ABSTRACT FROM AUTHOR]- Published
- 2015
42. Synthesis, Characterization and Biological Activity of Some New S-Substituted Derivatives of 5-(2-Chlorophenyl)-1,3,4-Oxadiazol-2-Thiol.
- Author
-
Aziz-ur-Rehman, Rasool, Shahid, Abbasi, M. Athar, Siddiqui, Sabahat Z., Sattar, Almas, Khan, Khalid Mohammed, Ahmad, Irshad, and Afzal, Saira
- Subjects
CHEMICAL synthesis ,THIOL synthesis ,CHEMICAL reactions ,ANTIBACTERIAL agents ,ACETAMIDE - Abstract
Molecules with multi-functional groups are being synthesized to acquire more potent molecules. Two series of S-substituted derivatives of 5-(2-chlorophenyl)-1,3,4-Oxadiazol-2-thiol (4) were synthesized and also evaluated for their biological activities. The 2-chlorobenzoic acid (1) was stepped up to ethyl 2-chlorobenzoate (2), 2-chlorobenzohydrazide (3) and 5-(2-chlorophenyl)-1,3,4- Oxadiazol-2-thiol (4). The molecule 4 was made to react with N-substituted-2-bromoacetamide, 6a-f, to yield N-substituted-2-((5-(2-chlorophenyl)-1,3,4-Oxadiazol-2-yl)sulfanyl)acetamide, 7a-f. Simultaneously, the compound 4 was converted to 2-(5-(2-chlorophenyl)-1,3,4-Oxadiazol-2- ylthio)acetohydrazide (9) which on reaction with different aldehydes, 10a-g, resulted N'-substituted- 2-(5-(2-chlorophenyl)-1,3,4-Oxadiazol-2-ylthio)acetohydrazide, 11a-g. The proposed structures of the molecules were supported by spectral analysis and the series 7a-f was found to be better antibacterial agents and lipoxygenase enzyme inhibitors as compared to 11a-g. [ABSTRACT FROM AUTHOR]
- Published
- 2015
43. Synthesis Leishmanicidal Activities of bis-Schiff Bases of Isatins.
- Author
-
Khan, Momin, Khan, Khalid Mohammed, Rahim, Fazal, Samreen, Perveen, Shahnaz, Karim, Aneela, mtiazuddin, and Choudhary, Muhammad Iqbal
- Subjects
- *
ISATIN , *SCHIFF bases , *CHEMICAL derivatives , *ALDIMINES , *BIOLOGICAL assay - Abstract
Twenty seven (27) derivatives of bis-Schiff bases of isatins 1-27 were studied for their leishmanicidal potential. Out of twenty seven (27) analogs, five exhibited varying degree of leishmanicidal activity with IC50 values 44.86 ± 0.66, 65.27 ± 0.38, 76.58 ± 0.30, 46.51 ± 0.36, and 84.05 ± 0.23 μM, and rests of the compounds showed no leishmanicidal activity. [ABSTRACT FROM AUTHOR]
- Published
- 2015
44. Synthesis of Benzophenone Hydrazone Analogs and their DPPH Radical Scavenging and Urease Inhibitory Activities.
- Author
-
Khan, Khalid Mohammed, Rahim, Fazal, Khan, Ajmal, Ali, Sajjad, Taha, Muhammad, Saad, Syed Muhammad, Khan, Momin, Najeebullah, Shaikh, A., Perveen, Shahnaz, and Choudhary, Muhammad. Iqbal
- Subjects
- *
HYDRAZONES , *BENZOPHENONES , *CHEMICAL synthesis , *ANTIOXIDANTS , *UREASE - Abstract
Benzophenone hydrazone analogs 1-25 were synthesized and evaluated for antioxidant (DPPH radical scavenging), and urease inhibitory activities. Out of twenty-five analogs, compounds 8, 23, and 1 showed potent free radical scavenging activities with IC50 values 19.45 ± 1.25, 21.72 ± 1.49, and 26.0 ± 0.52 μM, respectively, while compound 8 (IC50 = 36.36 ± 0.94 μM), and 15 (IC50 = 55.5 ± 0.69 μM), showed good to moderate urease inhibitory potential. [ABSTRACT FROM AUTHOR]
- Published
- 2015
45. Pulicaria undulata: A Potential Phytochemical, Antimicrobial and Antioxidant Source.
- Author
-
Ajaib, Muhammad, Mati-ur-Rehman, Aatiqa, Khan, Khalid Mohammed, Perveen, Shahnaz, and Shah, Shazia
- Subjects
PHYTOCHEMICALS ,ANTI-infective agents ,CHLOROFORM ,PETROLEUM industry ,ANTIFUNGAL agents - Abstract
Phytochemical analysis, antimicrobial and antioxidant activities of petroleum ether, chloroform, methanol and aqueous extracts of the plant Pulicari aundulata (L.) C. A. Myer was carried out by using various techniques. The phytochemical analysis of the plant material showed the presence of alkaloids (15.53%), flavonoids (15.81%), phenols (18.91%), saponins (12.13%) and tannins (6.42%). Antimicrobial activity indicated that methanolic extract showed maximum antibacterial potential 44 ± 3.05 mm against P. aureginosa, chloroform extract 39 ± 0.5 mm and petroleum ether extract 37 ± 2.6 mm against S. aureus. The petroleum ether extract showed maximum zone of inhibition of antifungal potential by A. niger which was 32 ± 1.1 mm. The MIC assay was carried out for further analysis which showed the MIC value of methanolic extract was 0.051 ± 0.1 at 1 mg/ml against P. aureginosa and the MIC value against A. niger was 0.52 ± 0.22 at 0.2 mg/ml. Antioxidant potential was determined by using four methods 1,1-diphenyl-2- picrylhydrazyl radical scavenging activity (DPPH), total antioxidant activity (TAA), total phenolic contents (TPC) and metal chelating activity (MC). The aqueous extract showed highest value of % DPPH 73.55% at 250 μg/ml and the IC50 value of aqueous extract was 214.45 ± 0.67. The maximum values of total antioxidant activity (3.607 ± 0.33) was observed by aqueous extract, total phenolic content (11.76 ± 2.1) by chloroform and metal chelating activity (64.19 ± 1.5) by aqueous extract. [ABSTRACT FROM AUTHOR]
- Published
- 2015
46. Study of Vanadium Complexes as Novel Inhibitors of Bacillus Pasteurii and Canavalia Ensiformis Urease Enzyme.
- Author
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Lodhi, Muhammad Arif, Ashiq, Uzma, Jamal, Rifat Ara, and Khan, Khalid Mohammed
- Subjects
VANADIUM ,BACILLUS (Bacteria) ,CANAVALIA ensiformis ,UREASE ,ENZYME kinetics ,LIGANDS (Chemistry) - Abstract
Oxovanadium(IV) complexes with aroylhydrazine ligands have been synthesized. Structural elucidation of synthesized complexes is carried out with the help of various physical, chemical and spectral analysis. Dimeric nature of synthesized complexes further characterized by effective magnetic moments, spectral, conductance, CHN and metal analysis. In the current study we examined 1c to 10c vanadium (IV)-aroylhydrazine complexes for their mechanism of inhibition with the nickel containing active sites of Canavalia ensiformis (Jack bean) and Bacillus pasteurii ureases. Inhibition of both urease enzymes by compounds 1c-10c are depends on concentration. Lineweaver- Burk as well as Dixon plots and their secondary replots indicated that the mechanisms of inhibition exhibited by vanadium complexes 1c-10c are very diverse. The Ki values ranging from 15.1-79.3 μM for Canavalia ensiformis urease while for Bacillus pasteurii urease 25.2-123.7 μM. The model presented here is evidenced by biochemical enzyme kinetics data. Efforts are made to obtain significant approach into the pharmacophore needs of urease. The high affinity of these vanadium complexes along with their safe profile against plants could make them promising lead candidates and provides fertile ground for future research. [ABSTRACT FROM AUTHOR]
- Published
- 2015
47. N-Sulfonated Derivatives of 2,3-Xylidine as Suitable Antibacterial Agents.
- Author
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Abbasi, Muhammad Athar, Sheeza, Anam, Aziz-ur-Rehman, Siddiqui, Sabahat Zahra, Khan, Khalid Mohammed, Malik, Rabia, and Ahmad, Irshad
- Subjects
DIMETHYLANILINE ,ANTIBACTERIAL agents ,CHEMICAL derivatives ,SULFONATES ,CHEMICAL inhibitors - Abstract
The objective of the current research effort was to unravel the antibacterial potential of some newly synthesized sulfonamides. 2,3-Dimethylaniline (2,3-xylidine, 1) was reacted with different sulfonyl chlorides (2a-g) under dynamic control of pH (9-10) in aqueous alkaline medium to generate a series of N-sulfonated derivatives of 2,3-xylidine (3a-g). The plausible structures of the synthesized derivatives were corroborated by contemporary spectral techniques e.g. IR,
1 H-NMR and EIMS. Moreover, N-sulfonated derivatives were screened against different gram negative and positive bacterial strains to evaluate their inhibitory potential. They depicted good to moderate inhibitory potential, especially, N-(2,3-dimethylphenyl)methanesulfonamide (3a), N-(2,3- dimethylphenyl)-4-methylbenzenesulfonamide (3b), N-(2,3-dimethylphenyl)-4- bromobenzenesulfonamide (3d) and N-(2,3-dimethylphenyl)naphthalene-2-yl-sulfonamide (3f) were amongst the potent inhibitors as compared to standard; Ciprofloxacin. [ABSTRACT FROM AUTHOR]- Published
- 2015
48. The Long Chain Alcohols of the n-hexane Fraction of Water Hyacinth (Eichhornia crassipes): Extraction, Estimation, GC-MS Analysis and Antimicrobial Activity.
- Author
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Hussain, Zahid, Khan, Khalid Mohammed, Perveen, Shahnaz, Zaman, Khair, Hayat, Ghazanfar, Karim, Aneela, Khan, Momin, and Khan, Shad Ali
- Subjects
- *
ALCOHOLS (Chemical class) , *WATER hyacinth , *ANTI-infective agents , *HEXANE , *ALIPHATIC hydrocarbons - Abstract
Oily fraction was extracted from the water hyacinth (Eichhornia crassipes) using nhexane by both cold and hot extraction in 5.5 ± 0.05% and 9.30 ± 0.05%, respectively, however, no difference was found in the nature of the compounds extracted by the two processes. The analysis of this oil was carried out using GC-FID and GC-MS in separate experiments and the nature of the compounds was investigated by library matching of the spectra obtained through GC-MS. This extract was found to contain 33.267% of the nonadecan-4-ol and 20.51% of a long chain ketone in addition to various quantities of the long chain nitrogenous compounds. The antibacterial activity of the extract was investigated against eight pathogenic bacteria and fungus Candida albican using disc diffusion method. The extract was found to be highly active against all tested bacterial strains except S. typhi. For most of the strains the activity of the extract was near the reference. Ciprofloxacin, clotrimazole and erythromycin were used as reference antibiotics. [ABSTRACT FROM AUTHOR]
- Published
- 2015
49. Antioxidant and Antimicrobial Activities of Helinus lanceolatus.
- Author
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Ajaib, Muhammad, Khan, Khalid Mohammed, Perveen, Shahnaz, and Shah, Shazia
- Subjects
- *
ANTIOXIDANTS , *ANTI-infective agents , *PETROLEUM , *METHANOL , *PEROXIDATION - Abstract
The extracts of petroleum ether, chloroform, methanol and aqueous of Helinus lanceolatus were tested for their antioxidant potential, antibacterial and antifungal activities. The results revealed that the methanolic extract showed the highest zone of inhibition 50 ± 1.15 mm against Escherichia coli and aqueous extract shows excellent inhibition for fungi Aspergillus niger 17 ± 2.6 mm. The water extract showed highest DPPH radical scavenging activity i.e. 91.8 ± 0.0.09% at a concentration of 500 μg/ml with IC50 value 12.29 ± 0.59 μg/ml relative to butylated hydroxyltoluene (BHT) having IC50 value 12.52 ± 0.89 μg/ml. Chloroform extract showed highest antioxidant activity 0.840 ± 0.13 μg/ml relative to standard 0.891 ± 0.13 μg/ml while the highest FRAP value i.e. 90.66 ± 4.54 TE μg/ml was shown by petroleum ether fraction. Methanolic extract also showed good value of inhibition of lipid peroxidation, i.e. 59.11 ± 0.12%. [ABSTRACT FROM AUTHOR]
- Published
- 2015
50. Antileishmanial Activities of Benzothiazole Derivatives.
- Author
-
Rahim, Fazal, Samreen, Taha, Muhammad, Muhammad Saad, Syed, Perveen, Shahnaz, Khan, Momin, Alam, Muhammad Tanveer, Khan, Khalid Mohammed, and Iqbal Choudhary, M.
- Subjects
BENZOTHIAZOLE ,AROMATIC compounds ,CHEMICAL derivatives ,LEISHMANIA ,TRYPANOSOMATIDAE - Abstract
Benzothiazole derivat ives 1-22 were synthesized from 2-aminothiophenol and all synthetic compounds were screened for in vitro antileishmanial activity. These compound showed different types activities against leishmania with IC
50 values ranging between 18.32 - 81.89 μM. Compound 2 (IC50 = 18.32 ± 0.18 μM), 5 (IC50 = 19.72 ± 0.32 μM), and 3 (IC50 = 21.87 ± 0.43 μM) were found to be the most act ive compounds among the series when compared to the standard (Pentamidine, IC50 = 5.09 ± 0.04 μM). Compounds 7 and 11 exhibited weak act ivit ies, while compounds 5, 6, 7, 10, 11, and 16 were also found act ive. However, remaining compounds were found to be inact ive against leishmania [ABSTRACT FROM AUTHOR]- Published
- 2015
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