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The present study aimed to investigate the enzymetic, non-enzymetic toxicity and antioxidant potential of a drug candidate 5-Benzyl-1,3,4-Oxadiazole-2-Thiol(OXPA) using computational tools and in vivo models. The binding pattern of it, with different toxicity/oxidative enzymes was predicted using software pkCSM, Protox- II, LAZAR, Mcule 1-Click Docking 3D-Ligand binding Site and best score obtained used as an evaluating criterion. After acute oral toxicity, in vivo. antioxidant and hepato protective activity was investigated on male wistar rats, segregated into four groups as control (NS), toxic (INH-RIF), standard (Silymerin) and sample (OXPA, 100mg/Kg) for 21days. Level of antioxidant enzymes / histopathology and serum biochemical parameters in liver and blood of treated rats was assessed by using scientific tools. In silico study reveal no profound toxicity parameters however, LD50 found to be 560mg/Kg while in vivo study declared it safe till 1000mg/Kg, as having no toxicity symptoms. Molecular interaction score with GTH reductase, s-transferase and significant in vivo antioxidant effect on catalase, SOD, TBARS enzymes and histopathological assessment, declare OXPA a good antioxidant having significant (P< 0.05) hepato protective activity. Results of in silico, in vivo studies declare the propensity of 5-Benzyl-1, 3, 4-oxadiazole-2-thiol as potential antioxidant, for further investigations as a drug. [ABSTRACT FROM AUTHOR]

2-Furoyl-1-piperazine (1) was treated with a series of alkyl/aryl sulfonyl chlorides (2a-i) under benignant conditions to obtain its N-sulfonated derivatives (3a-i). These compounds were screened for their antibacterial potential against pathogenic bacteria. The low Minimum Inhibitory Concentration (MIC) values of these molecules, in comparison of ciprofloxacin, demonstrated their high antibacterial potential. Cytotoxic activities were ascertained through their hemolytic potential and mild hemolytic profiles of these compounds proved them to be promising compounds for drug designing and development. [ABSTRACT FROM AUTHOR]

The synthetic methodology was initiated by reacting 1,4-benzodioxane-6-amine (1) with 2-bromoacetyl bromide (2) in aqueous alkaline media under dynamic pH control to get compound 2,3-dihydro-1,4-benzodioxin-6-yl-2- bromoacetamide (3). In the subsequent reactions, a variety of un/substituted-benzoic acids (4a-k), through a succession of three steps, was converted into respective oxadiazole nucleophiles, 7a-k. Finally, the targeted molecules, 8a-k, were obtained by reacting 7a-k with electrophile 3 in an aprotic polar solvent. These compounds were corroborated by spectral characterization like IR, EI-MS, ¹H-NMR, and CHN analysis data. These molecules were screened for their antibacterial potential and most of them exhibited a potent activity. Moreover, their cytotoxicity was profiled through hemolytic activity and it was observed that majority of them was very modest in toxicity. [ABSTRACT FROM AUTHOR]

1,2,4-triazoles are a major group of heterocyclic compounds. In the current work, a concise library of such triazoles synthesized through a multistep protocol. The synthesis involved hydrazinolysis of ethyl-2-(p-Cl-phenoxy) acetate followed by reflux with phenyl isothiocyanate to yield the intermediate 2-[2-(p-Cl-phenoxy)acetyl)-N-phenylhydrazinecarbothioamide. This intermediate was then cyclized to form 5-[p-(Cl-phenoxy)-methyl]-4-phenyl-4H-1,2,4-triazole-3-thiol (the parent moiety) at alkaline pH. In parallel, 3-bromopropionyl bromide was reacted with a series of phenylamines to yield N-(substituted-phenyl)bromopropanamides. In the final step, N-substitution of 5-[p-(Cl-phenoxy)-methyl]-4-phenyl-4H-1,2,4-triazole-3-thiol was carried out with N-(substituted-phenyl)bromopropanamides to give desired library of 3-[5-[(p-Cl-phenoxy)-methyl]-4-phenyl-4H-1,2,4-triazole-3-ylthio]-N-(substituted-phenyl) propanamides (8a-l). The prepared moieties were identified via IR, NMR, & EIMS and evaluated for urease and antiproliferative activities. 3-[5-[(p-Cl-phenoxy)-methyl]-4-phenyl-4H-1,2,4-triazole-3-ylthio]-N-(3-methylphenyl) propanamide 8k, was found to be most prominent hit as urease inhibitor (IC50= 42.57± 0.13 µM) using thiourea as standard (IC50= 21.25±0.15µM). The interaction of 8k with urease were studied using docking studies. Antiproliferative activity results showed 8k as promising candidates and rest of the synthesized derivatives were found to be moderately anti-proliferative. Molecular docking results also displayed 8k, 8h, and 8c as potential hits for further study. [ABSTRACT FROM AUTHOR]

In the presented work, 2,3-dihydro-1,4-benzodioxin-6-amine (1) was reacted with 4-chlorobenzenesulfonyl chloride (2) in presence of aqueous basic aqueous medium to obtain 4-chloro-N-(2,3-dihydro-1,4-benzodioxin-6- yl)benzenesulfonamide (3). In parallel, various un/substituted anilines (4a-l) were treated with bromoacetyl bromide (5) in basified aqueous medium to obtain corresponding 2-bromo-N-(un/substituted)phenylacetamides (6a-l) as electrophiles. Then the compound 3 was finally reacted with these electrophiles, 6a-l, in dimethylformamide (DMF) as solvent and lithium hydride as base and activator to synthesize a variety of 2-[[(4-chlorophenyl)sulfonyl](2,3-dihydro- 1,4-benzodioxin-6-yl)amino]-N-(un/substituted)phenylacetamides (7a-l). The synthesized compounds were corroborated by IR, 1H-NMR and EI-MS spectral data for structural confirmations. These molecules were then evaluated for their antimicrobial and antifungal activities along with their %age hemolytic activity. Some compounds were found to have suitable antibacterial and antifungal potential, especially the compound 2-[[(4-chlorophenyl)sulfonyl](2,3-dihydro-1,4- benzodioxin-6-yl)amino]-N-(3,5-dimethylphenyl)acetamide (7l) exhibited good antimicrobial potential with low value of % hemolytic activity. [ABSTRACT FROM AUTHOR]

A series of propanamide compounds 6a-l was derived by N-substitution reactions, encompassing tosyl, piperidine and 1,3,4-oxadiazole moieties. The intended array of compounds 6a-l was afforded by a series of five steps reaction scheme. 1-Tosylpiperidin-4-carboxylate (1) was synthesized by the reaction of tosyl chloride (a) with ethyl isonipecotate (b) under mild basic conditions. Compound 1 was subjected to nucleophillic substitution by hydrazine to synthesize 1-tosylpiperidin-4-carbohydrazide (2). The compound, 5-(1-tosylpiperidin-4-yl)-1,3,4-oxadiazole-2-thiol (3) was synthesized by intermolecular cyclization of compound 2 by CS2 under strong basic conditions. The target compounds, 6a-l, were finally synthesized from 3 by reacting with different electrophiles, 5a-l, in an aprotic polar solvent with sodium hydride as an activator. The different propanamoyl electrophiles, 5a-l, were synthesized by the reaction of different aromatic and aliphatic amines, 4a-l, with 3-bromopropionyl chloride under mild basic conditions. The structural elucidation was carried out using modern spectroscopic techniques including IR, 1H-NMR and EI-MS. The antibacterial potential of synthesized compounds was assessed against five bacterial strains. Compounds 6a, 6c, 6d, 6e and 6f were found to be potent antibacterial agents. [ABSTRACT FROM AUTHOR]

In the planned research work, the nucleophilic substitution reaction of 1-[(E)-3-phenyl-2-propenyl]piperazine (1) was carried out with different sulfonyl chlorides (2a-g) at pH 9-10 to synthesize its different N-sulfonated derivatives (3a-g). The structures of the synthesized compounds were characterized by their proton-nuclear magnetic resonance (1HNMR), carbon-nuclear magnetic resonance (13C-NMR) and Infra Red (IR) spectral data, along with CHN analysis. The inhibition potential of the synthesized molecules was ascertained against two bacterial pathogenic strains i.e. Bacillus subtilis and Escherichia coli. It was inferred from the results that some of the compounds were very suitable inhibitors of these bacterial strains. Moreover, their cytotoxicity was also profiled and it was outcome that most of these molecules possessed moderate cytotoxicity. [ABSTRACT FROM AUTHOR]

Following the Claisen Schmidt condensation a series of chalcone, their allylidene derivatives and metallic complexes were produced and subsequently screened for antibacterial assay. The precursors were simple acetophenone and different substituted aryl benzaldehydes; which were made to react in basic ethanolic conditions. The structure of synthesized targets was established by IR, ¹H-NMR and EIMS data. The antibacterial statistics showed that most of the bacterial strains particularly S. typhi and E. coli were potently inhibited by majority of the compounds like 3c, 5c, 7a & 7c. This structure activity relationship studies showed that these molecules possessed p-methoxy substituents in their framework and found active in rupturing the cell wall. These molecules might serve as potential drug candidates for future drug discovery and design. The presented manuscript highlights the pharmacological diversity of chalcones holding allylidene moiety and Zn+2 complexes. [ABSTRACT FROM AUTHOR]

A series of new compounds (5a-q), derived from 5-(1-(4-nitrophenylsulfonyl) piperidin-4-yl)-4-phenyl-4H- 1,2,4-triazole-3-thiol (3) were proficiently synthesized to evaluate their biological activities. 1-(4-Nitrophenylsulfonyl) piperidine-4-carbohydrazide (2) was refluxed with phenylisothiocyanate to yield an adduct which was cyclized to compound 3 by reflux reaction with 10% potassium hydroxide. The targeted compounds 5a-q, were synthesized by stirring alkyl/aralkyl halides (4a-q) and compound 3 in a polar aprotic solvent. ¹H-NMR, 13C-NMR, EI-MS and IR spectral techniques were employed to confirm the structures of all the synthesized compounds. The compounds were biologically evaluated for BSA binding studies followed by anti-bacterial, anti-inflammatory and acetylcholinesterase (AChE) activities. The active sites responsible for the best AChE inhibition were identified through molecular docking studies. Compound 5e bearing 4-chlorobenzyl moiety found most active antibacterial and anti-inflammatory agent among the synthesized compounds. The whole library of synthesized compounds except compounds 5d and 5f was found highly active for AChE inhibition and recommended for in vivo studies so that their therapeutic applications may come in utilization. [ABSTRACT FROM AUTHOR]

The current research was commenced by reaction of 1,4-benzodioxane-6-amine (1) with 4- nitrobenzenesulfonyl chloride (2) in the presence of aqueous base under dynamic pH control at 9 to yield N-(2,3-dihydro- 1,4-benzodioxin-6-yl)-4-nitrobenzenesulfonamide (3) which was further reacted with a series of alkyl/aralkyl halides (4a-i) in polar aprotic solvent using catalytic amount of lithium hydride which acts as base to afford some new Nalkyl/aralkyl-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-nitrobenzenesulfonamides (5a-i). The projected structures of all the synthesized derivatives were characterized by contemporary techniques i.e., IR, ¹H-NMR and EIMS. The biofilm Inhibitory action of all synthesized molecules was carried out against Escherichia coli and Bacillus subtilis. It was inferred from their results that 5f and 5e exhibited suitable inhibitory action against the biofilms of these bacterial strains. Moreover, their cytotoxicity was also checked and it was concluded that these synthesized molecules displayed docile cytotoxicity. [ABSTRACT FROM AUTHOR]

A series of 1, 2, 4-triazole derivatives bearing piperidine moiety has been introduced as new anti-diabetic drug candidates with least cytotoxicity. p-Chlorophenylsulfonyl chloride (1) and ethyl nipecotate (2) were the starting reagents that resulted into corresponding 3,4,5-trisubstituted-1,2,4-triazole (6) through a series of steps. A series of electrophiles, 9a-e, were synthesized by reacting 4-bromobutyryl chloride (7) with differently substituted aromatic amines (8a-e) under basic aqueous medium. Target derivatives, 10a-e, were synthesized by the reaction of compound 6 with N-aryl-4-bromobutanamides (9a-e) in an aprotic solvent. Structures of all the derivatives were verified by spectroscopic analysis using IR, ¹H-NMR, 13C-NMR and EIMS. Most of the derivatives revealed moderate to good α-glucosidase inhibitory activity with reference to acarbose. The moderate hemolytic potential demonstrated least toxicity. [ABSTRACT FROM AUTHOR]

In the study presented here, the nucleophilic substitution reaction of 5-[3-(1H-indol-3-yl)propyl]-1,3,4- oxadiazol-2-ylhydrosulfide was carried out with different alkyl/aralkyl halides (5a-r) to form its different S-substituted derivatives (6a-r), as depicted in scheme 1. The structural confirmation of all the synthesized compounds was done by IR, ¹H-NMR, 13C-NMR and CHN analysis data. Bacterial biofilm inhibitory activity of all the synthesized compounds was carried out against Bacillus subtilis and Escherichia coli. The anticancer activity of these molecules was ascertained using anti-proliferation (SRB) assay on HCT 116 Colon Cancer Cell lines while the cytotoxicity of these molecules was profiled for their haemolytic potential. From this investigation it was rational that most of the compounds exhibited suitable antibacterial and anticancer potential along with a temperate cytotoxicity. [ABSTRACT FROM AUTHOR]

The aims of the present investigation were to assess the antibacterial, antifungal, enzyme inhibition and hemolytic activities of various fractions of Rhynchosia pseudo-cajan Cambess. The methanolic extract of the plant was dissolved in the water (distilled) and then partitioned with the n-hexane, chloroform, EtOAc and n-BuOH sequentially. Antibacterial activity was checked against Escherichia coli, Pasturella multocida, Bacillus subtilis and Staphylococcus aureus by the disc diffusion method using streptomycin sulphate, a standard antibiotic, as positive control. Chloroform and ethyl acetate soluble fractions showed good activity against Escherichia coli, Bacillus subtilis and Staphylococcus aureus. These fractions also showed good MIC values. The n-butanol soluble and remaining aqueous fraction also showed good activity against some strains. Antifungal activity was studied against four fungi i.e. Aspergillus niger, Aspergillus flavus, Ganoderma lucidum and Alternaria alternata by the disc diffusion method using fluconazole, a standard antifungal drug, as positive control. Chloroform, n-butanol and ethyl acetate soluble fraction showed good activity only against G. lucidum. Enzyme inhibition studies were done against four enzymes i.e. α-glucosidase, butyrylcholinesterase, acetyl cholinesterase and lipoxygenase. Aqueous fraction possessed very good activity against α- glucosidase, even greater than acarbose, a reference standard drug. Its IC50 value was found as 29.81±0.12 µg/ml as compared to acarbose having IC50 38.62±0.04 µg/ml. Chlroform and ethyl acetate soluble fractions also showed good activity against α-glucosidase. Ethyl acetate soluble and remaining aqueous fractions showed good activity against lipoxygenase. All the studied fractions showed very less toxicity i.e. <2.5%. [ABSTRACT FROM AUTHOR]

The present study comprises the synthesis of a new series of benzenesulfonamides derived from N-sulfonation of 2-(4-methoxyphenyl)-1-ethanamine (1). The synthesis was initiated by the reaction of 2-(4-methoxyphenyl)-1-ethanamine (1) with benzenesulfonyl chloride (2), to yield N-(4-methoxyphenethyl)benzenesulfonamide (3). This parent molecule 3 was subsequently treated with various alkyl/aralkyl halides (4a-j) in N,N-dimethylformamide (DMF) and in the presence of a weak base lithium hydride (LiH) to obtain various N-(alkyl/aralkyl)-N-(4-methoxyphenethyl) benzenesulfonamides (5a-j). The characterization of these derivatives was carried out by spectroscopic techniques like IR, ¹H-NMR, and 13C-NMR. Elemental analysis also supported this data. The biofilm inhibitory action of all the synthesized compounds was carried out on Escherichia coli and some of the compounds were identified to be very suitable inhibitors of this bacterial strain. Furthermore, the molecules were also tested for their cytotoxicity behavior to assess their utility as less cytotoxic therapeutic agents. [ABSTRACT FROM AUTHOR]

Heterocyclic chemistry is an important field of organic chemistry due to therapeutic potential. The minor modification in the structure of poly-functional compounds has great effect on therapeutic ability. In the presented research work, substituted 1,3,4-oxadiazole derivatives, 8a-p, have been synthesized by the reaction of 1-(4- bromomethylbenzenesulfonyl)-3-methylpiperidine (7) and 5-substituted-1,3,4-oxadiazole-2-thiol (4a-p). The 5-substituted-1,3,4-oxadiazole-2-thiol were synthesized by converting carboxylic acids correspondingly into esters, hydrazides and oxadiazoles. Secondly the electrophile, 1-(4-Bromomethylbenzenesulfonyl)-3-methylpiperidine (7), was prepared by the reaction of 3-methylpiperidine with 4-bromomethylbenzenesulfonyl chloride in the presence of water and Na2CO3 under pH of 9-10. The compounds were structurally corroborated through spectroscopic data analysis of IR, EI-MS and 1H-NMR. The screening for antibacterial activity revealed the compounds to be moderate to excellent inhibitors against bacteria under study. Anti-enzymatic activity was assessed against urease enzyme and 1-{[4-({[5-(3-nitrophenyl)-1,3,4-oxadiazol-2-yl]sulfanyl}methyl)phenyl]sulfonyl}-3-methylpiperidine (8d) was the most active one. [ABSTRACT FROM AUTHOR]

The present investigation was undertaken to evaluate the antibacterial, antifungal and hemolytic activities of organic and aqueous fractions of Fumaria indica, Dicliptera bupleuroides and Curcuma zedoaria. The methanolic extracts of the plants were dissolved in the water (distilled) separately and then partitioned with the n-hexane, CHCl3, EtOAc and n-BuOH sequentially. Antibacterial activity was checked against Escherichia coli, Pasturella multocida, Bacillus subtilis and Staphylococcus aureus by the disc diffusion method using streptomycin sulphate, a standard antibiotic, as positive control. Antifungal activity was studied against four fungi i.e. Aspergillus niger, Aspergillus flavus, Ganoderma lucidum and Alternaria alternata by the disc diffusion method using fluconazole, a standard antifungal drug, as positive control. It was revealed that aqueous fraction of F. indica showed very good antibacterial activity against P. multocida with zone of inhibition 26mm and MIC of 98µg/mL. Its CHCl3 and n-BuOH fractions also displayed good results. Its CHCl3 fraction showed good antifungal activity against G. lucidum with zone of inhibition 24mm and MIC of 115µg/mL. Other polar fractions of F. indica showed good activity against somefungal strains. The CHCl3 and EtOAc fractions of D. bupleuroides displayed good antibacterial activity against some bacterial strains. Its EtOAc fraction showed good antifungal activity only against G. lucidum. The CHCl3 fraction of C. zedoaria showed good activity against all studied bacterial strains, while its EtOAc and n-BuOH fractions displayed good results against some bacterial strains. None of the fractions of C. zedoaria displayed antifungal activity against the under test strains. All the studied fractions of three plants showed very less toxicity except n-hexane fraction of D. bupleuroides which showed 79% toxicity. [ABSTRACT FROM AUTHOR]

In the current research work, a series of new N-(alkyl/aralkyl)-N-(2,3-dihydro-1,4-benzodioxan-6-yl)-4- chlorobenzenesulfonamides has been synthesized by reacting 1,4-benzozzdioxan-6-amine (1) with 4- chlorobenzenesulfonyl chloride (2) to yield N-(2,3-dihydro-1,4-benzodioxan-6-yl)-4-chlorobenzenesulfonamide (3) which was further reacted with different alkyl/aralkyl halides (4a-n) to afford the target compounds (5a-n). Structures of the synthesized compounds were confirmed by IR, 1H-NMR, EI-MS spectral techniques and CHN analysis data. The results of enzyme inhibition showed that the molecules, N-2-phenethyl-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4- chlorobenzenesulfonamide (5j) and N-(1-butyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-chlorobenzenesulfonamide (5d), exhibited moderate inhibitory potential against acetylcholinesterase with IC50 values 26.25±0.11 µM and 58.13±0.15 µM respectively, whereas, compounds N-benzyl-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-chlorobenzenesulfonamide (5i) and N-(pentane-2-yl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-chlorobenzenesulfonamide (5f) showed moderate inhibition against a-glucosidase enzyme as evident from IC50 values 74.52±0.07 and 83.52±0.08 µM respectively, relative to standards Eserine having IC50 value of 0.04±0.0001 µM for cholinesterases and Acarbose having IC50 value 38.25±0.12 µM for a-glucosidase, respectively. [ABSTRACT FROM AUTHOR]

The research was aimed to unravel the enzymatic potential of sequentially transformed new triazoles by chemically converting 4-methoxybenzoic acid via Fischer's esterification to 4-methoxybenzoate which underwent hydrazinolysis and the corresponding hydrazide (1) was cyclized with phenyl isothiocyanate (2) via 2-(4-methoxybenzoyl)-N-phenylhydrazinecarbothioamide (3); an intermediate to 5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazol-3-thiol (4). The electrophiles; alkyl halides 5(a-g) were further reacted with nucleophilic S-atom to attain a series of S-alkylated 5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazole-3-thiols 6(a-g). Characterization of synthesized compounds was accomplished by contemporary spectral techniques such as FT-IR, 1H-NMR, 13C-NMR and EI-MS. Excellent cholinesterase inhibitory potential was portrayed by 3-(n-heptylthio)-5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazole; 6g against AChE (IC50; 38.35±0.62μM) and BChE (IC50; 147.75±0.67μM) enzymes. Eserine (IC50; 0.04±0.01μM) was used as reference standard. Anti-proliferative activity results ascertained that derivative encompassing long straight chain substituted at S-atom of the moiety was the most potent with 4.96 % cell viability (6g) at 25μM and with 2.41% cell viability at 50μMamong library of synthesized derivatives. In silico analysis also substantiated the bioactivity statistics. [ABSTRACT FROM AUTHOR]

Microwave and conventional techniques were employed to synthesize a novel array of compounds 7a-g with 1,2,4-triazole and piperidine rings having great biological importance. The microwave assisted method has a better operational scope with respect to time and yield comparative to the conventional method. 'H-NMR, l3C-NMR and IR techniques were employed to justify the structure of synthesized compounds. The antioxidant, butyrylcholinesterase inhibition and urease inhibition potential of every synthesized compound was evaluated. Every member of the synthesized series was found potent against mentioned activities. Compound 7g was the most active anti-urease agent having IC50(pM) value 16.5±0.09 even better than the thiourea with an IC50 (pM) value of 24.3±0.24. The better urease inhibition potential of 7g was also elaborated and explained by docking and bovine serum albumin (BSA) binding studies. [ABSTRACT FROM AUTHOR]

The aim of the present research work was synthesis of some 2-furyl[(4-aralkyl)-1-piperazinyl]methanone derivatives and to ascertain their antibacterial potential. The cytotoxicity of these molecules was also checked to find out their utility as possible therapeutic agents. The synthesis was initiated by reacting furyl(-1-piperazinyl)methanone (1) in N,N-dimethylformamide (DMF) and lithium hydride with different aralkyl halides (2a-j) to afford 2-furyl[(4-aralkyl)-1- piperazinyl]methanone derivatives (3a-j). The structural confirmation of all the synthesized compounds was done by IR, EI-MS, 1H-NMR and 13C-NMR spectral techniques and through elemental analysis. The results of in vitro antibacterial activity of all the synthesized compounds were screened against Gram-negative (S. typhi, E. coli, P. aeruginosa) and Gram-positive (B. subtilis, S. aureus) bacteria and were found to be decent inhibitors. Amongst the synthesized molecules, 3e showed lowest minimum inhibitory concentration MIC = 7.52±0.μg/mL against S. Typhi, credibly due to the presence of 2-bromobenzyl group, relative to the reference standard, ciprofloxacin, having MIC = 7.45±0.58μg/mL. [ABSTRACT FROM AUTHOR]

A number of novel 5-substituted-2-((6-bromo-3,4-methylenedioxybenzyl)thio)-1,3,4-Oxadiazole derivatives (6a-l) have been synthesized to evaluate their antibacterial activity. Using aryl/aralkyl carboxylic acids (1a-l) as precursors, 5-substituted-1,3,4-Oxadiazol-2-thiols (4a-l) were yielded in good amounts. The derivatives, 4a-l, were subjected to electrophilic substitution reaction on stirring with 6-bromo-3,4-methylenedioxybenzyl chloride (5) in DMF to synthesize the required compounds. All the synthesized molecules were well characterized by IR, 1H-NMR, 13C-NMR and EIMS spectral data and evaluated for antibacterial activity against some bacterial strains of Gram-bacteria. The molecule, 6d, demonstrated the best activity among all the synthesized molecules exhibiting weak to moderate inhibition potential. [ABSTRACT FROM AUTHOR]

An electrophile, N-(1,3-thiazol-2-yl)-2-bromoacetamide (3), was synthesized by the reaction of 1,3-thiazole-2-amine (1) and 2-bromoethanoyl bromide (2) in an aqueous medium. A series of carboxylic acids, 7a-j, were converted into 1,3,4-oxadiazole heterocyclic core, through a series of three steps. The final compounds, 8a-j, were synthesized by stirring 7a-j and 3 in an aprotic polar solvent. The structural elucidation of the synthesized compounds was supported by IR, EI-MS, 1H-NMR, and 13C-NMR spectral data. Title compounds were evaluated for enzyme inhibition against cholinesterases and α-glucosidase enzymes and their cytotoxic behavior was monitored using brine shrimp assay. The enzyme inhibitor potential of compounds was supported by molecular docking studies. [ABSTRACT FROM AUTHOR]

In this work, a new series of 2-[4-(2-furoyl)-1-piperazinyl]-N-aryl/aralkyl acetamides has been synthesized and evaluated for their antibacterial potential. The synthesis was initiated by the reaction of different aryl/aralkyl amines (1a-u) with 2-bromoacetylbromide (2) to obtain N-aryl/aralkyl-2-bromoacetamides (3a-u). Equimolar quantities of different N-aryl/aralkyl-2-bromoacetamides (3a-u) and 2-furoyl-1-piperazine (4) was allowed to react in acetonitrile and in the presence of K2CO3, to form 2-[4-(2-furoyl)-1-piperazinyl]-N-aryl/aralkyl acetamides (5a-u). The structural elucidation was done by EI-MS, IR and 1H-NMR techniques of all the synthesized compounds. All of the synthesized molecules were active against various Gram positive and Gram negative bacterial strains. Among them 5o and 5c showed very excellent MIC values. The cytotoxicity of the molecules was also checked to find their utility as possible therapeutic agents, where 5c (0.51%) and 5g (1.32%) are found to be least toxic in the series. [ABSTRACT FROM AUTHOR]

The present study describes the development and validation of a simple high performance liquid chromatographic method for the determination of a novel drug candidate, 5-[(4-chlorophenoxy) methyl]-1, 3, 4-oxadiazole-2-thiol. The stability-indicating capacity of the method was evaluated by subjecting the compound's solution to hydrolytic, oxidative, photolytic, transition metal- and thermal- stress. The chromatographic separation was achieved over a C18 column (Promosil, 5 μm, 4.60 × 250 mm), maintained at 25°C, using an isocratic mobile phase comprising a mixture of acetonitrile and acidified water of pH 2.67 (1:1, v/v), at a flow rate of 1.00 mL/min and detection using a fluorescent light detector (excitation at 250 nm and emission at 410 nm). The Beer's law was followed over the concentration range 2.50-50.00 μg/mL. The recovery (98.56-100.19%, SD <5%), intraday accuracy and precision (97.31-100.81%, RSD <5%), inter-day accuracy and precision (97.50-100.75%, RSD <5%) and intermediate accuracy and precision (98.10-99.91%, RSD <5%) indicated that the method was reliable, repeatable, reproducible and rugged. The resolution and selectivity factors of the compound's peak from the nearest resolving peak, particularly in case of dry heat and copper metal stress, were found to be greater than 2 and 1, respectively, which indicated specificity and selectivity. The compound was extensively decomposed in alkaline-hydrolytic, oxidative, metal- and dry heat- stress. However, the compound in acidic and neutral conditions was resistant to photolysis. The results of the present study indicate that the developed method is specific, selective, sensitive and suitable, hence, may be used for quality control, stability testing and preformulation studies. [ABSTRACT FROM AUTHOR]

The synthetic methodology is carried out in multistep which was initiated as phase I by utilizing Fischer esterification methodology of 2-phenylacetic acid (1) to ethyl-2-phenylacetate (2). The ester was reacted with hydrazine hydrate form 2-phenylacetohydrazide (3) which underwent ring closure with carbon disulfide in alcoholic base to achieve 5-benzyl-1,3,4-oxadiazole-2-thiol (4). Phase II, involved the reaction of electrophiles with 2- bromoacetylbromide (5) with arylated/arenylated amines (6a-e) in aqueous alkaline medium under vigorous shaking to generate N-substituted-2-bromoacetamides (7a-e). Finally in phase III, the parent oxadiazole reacted with N-substituted-2-bromoacetamides and in DMF/LiH to yield 2-[(5-benzyl-1,3,4-oxadiazole-2yl)sulfanyl]-N-(arylated/arenylated) acetamides (8a-e). All the derivatives were screened for their anti-enzymatic potential against acetyl/butyrylcholinesterase and lipoxygenase and for the antibacterial activity. They were found to be weak enzyme inhibitors and also possessed weak antibacterial action with the exception of 8e, which demonstrated prominent anti - enzymatic and antibacterial activity, which may be attributed to the presence of 3,4-dimethoxyphenylacetamide moiety. The LD50 data revealed that most of the N-substituted derivatives were found to be less cytotoxic. [ABSTRACT FROM AUTHOR]

Heterocyclic molecules have been frequently investigated to possess various biological activities during the last few decades. The present work elaborates the synthesis and enzymatic inhibition potentials of a series of sulfonamides. A series of 1-arylsulfonyl-4-Phenylpiperazine (3a-n) geared up by the reaction of 1-phenylpiperazine (1) and different (un)substituted alkyl/arylsulfonyl chlorides (2a-n), under defined pH control using water as a reaction medium. The synthesized molecules were characterized by 1H-NMR, 13C-NMR, IR and EI-MS spectral data. The enzyme inhibition study was carried on α-glucosidase, lipoxygenase (LOX), acetyl cholinesterase (AChE) and butyryl cholinesterase (BChE) enzymes supported by docking simulation studies and the IC50 values rendered a few of the synthesized molecules as moderate inhibitors of these enzymes where, the compound 3e exhibited comparatively better potency against α-glucosidase enzyme. The synthesized compounds showed weak or no inhibition against LOX, AChE and BChE enzymes. [ABSTRACT FROM AUTHOR]

The undertaken research was initiated by transforming 2-(1H-Indol-3-yl)acetic acid (1) in catalytic amount of sulfuric acid and ethanol to ethyl 2-(1H-Indol-3-yl)acetate (2), which was then reacted with hydrazine monohydrate in methanol to form 2-(1H-Indol-3-yl)acetohydrazide (3). Further, The reaction scheme was designed into two pathways where, first pathway involved The reaction of 3 with substituted aromatic aldehydes (4a-o) in methanol with few drops of glacial acetic acid to generate 2-(1H-Indol-3-yl)-N-[(un)substitutedphenylmethylidene]acetohydrazides (5a-o) and in second pathway 3 was reacted with acyl halides (6a-e) in basic aqueous medium (pH 9-10) to afford 2-(1H-Indol-3-yl)- N-[(un)substitutedbenzoyl/2-thienylcarbonyl]acetohydrazides (7a-e). All The synthesized derivatives were characterized by IR, EI-MS and 1H-NMR spectral techniques and evaluated for their anti-bacterial potentials against Gram positive and Gram negative bacterial strains and it was found that compounds 7a-d exhibited antibacterial activities very close to standard Ciprofloxacin. The synthesized derivatives demonstrated moderate to weak antienzymatic potential against α-Glucosidase and Butyrylcholinesterase (BChE) where, compounds 7c and 5c exhibited comparatively better inhibition against these enzymes respectively. Compounds 7a, 7d and 7e showed excellent antienzymatic potentials against Lipoxygenase (LOX) and their IC50 values were much lower than the reference standard Baicalein. Enzyme inhibitory activities were also supported by computational docking results. Compounds 5c, 7a, 7b and 7c also showed low values of % hemolytic activity as well, showing that these molecules were not toxic, indicating that these molecules can be utilized as potential therapeutic agents against inflammatory ailments. [ABSTRACT FROM AUTHOR]

A facile method has been implemented for the synthesis of different N-substituted sulfamoylacetamides by reacting 4-acetamidobenzenesulfonyl chloride (1) with different alkyl/aralkyl/aryl amines (2a-q) in basic aqueous media under controlled pH to afford -[(Substitutedsulfamoyl) phenyl]acetamides (3a-q) which were confirmed through spectral analysis like FT-IR, EIMS and 1H-NMR. Moreover, the synthesized derivatives were screened against α-Chymotrypsin. The enzyme inhibitory results revealed that most of the synthesized compounds were found to be moderate enzyme inhibitors. [ABSTRACT FROM AUTHOR]

The purpose of the research work was to examine the in vitro antioxidant activity of the different aqueous and organic fractions of Lonicera quinquelocularis Hardwicke. The methanol extract was dissolved in distilled water and fractioned with n-hexane, chloroform, ethyl acetate and n-butanol, successively. The antioxidant potential of the remaining aqueous and organic fractions was determined by using 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) scavenging activity, total antioxidant activity, ferric reducing antioxidant power (FRAP) assay, ferric thiocyanate assay and total phenolics method. Among these fractions ethyl acetate fraction displayed the maximum antioxidant activity with IC50 of (11.13±0.12µg/ml). It also exhibited the highest total antioxidant activity (0.595±0.00), FRAP value (128.2±4.54µg/mL) and total phenolic contents (66.89±7.73µg/g) as compared to other organic fractions. Phytochemical investigation of the above mentioned fractions showed the presence of flavanoids, phenolics, terpenoids, sugars, alkaloids, tannins, saponins and cardiac glycosides in appreciable amounts, which have major contribution towards antioxidant activity. [ABSTRACT FROM AUTHOR]

The purpose of the present investigation was to assess the enzyme inhibition, antifungal, antibacterial and hemolytic activities of various fractions of Colebrookia oppositifolia Smith. The MeOH extract of plant was dissolved in dist. water and partitioned with n-hexane, CHCl3, EtOAc and n-BuOH sequentially. Enzyme inhibition studies were done against four enzymes i.e. α-glucosidase, butyrylcholinesterase, acetyl cholinesterase and lipoxygenase. Ethyl acetate fraction possessed very good activity against a-glucosidase (IC50 57.38±1.23µg/mL). CHCl3 fraction displayed good activity against a-glucosidase and lipoxygenase while moderate activity against butyryl cholinesterase. EtOAc fraction displayed good activity against lipoxygenase. Antifungal activity was studied against four fungi i.e. Aspergillus niger, Aspergillus flavus, Ganoderma lucidum and Alternaria alternata by the disc diffusion method using fluconazole, a standard antifungal drug, as positive control. Aqueous fraction displayed good activity against G. lucidum and A. flavus. Antibacterial activity was checked against Staphylococcus aureus, Bacillus subtilis, Pasturella multocida and Escherichia coli by the disc diffusion method using streptomycin sulphate, a standard antibiotic, as positive control. Chloroform, ethyl acetate and aqueous fraction showed good activity against E. coli. Chloroform fraction showed good activity against B. subtilis. Ethyl acetate fraction showed good activity against the P. multocida. All the studied fractions showed very less toxicity i.e. < 7%. [ABSTRACT FROM AUTHOR]

The various p-substituted benzenesulfonyl chlorides (2a-e) were treated with (3,4-methylenedioxy) benzylamine (1) in the presence of aqueous Na2CO3 solution to synthesize N-(3,4-methylenedioxybenzyl)-4-substitutedbenzenesulfonamides (3a-e). The synthesized molecules were further converted into corresponding Nethyl/benzyl/4-flourobenzyl-N-(3,4-methylenedioxybenzyl)-4-substitutedbenzenesulfonamides (7a-e, 8a-e, 9a-e) on reaction with ethyl iodide (4), benzyl chloride (5) and 4-flourobenzyl chloride (6) in the presence of sodium hydride using N,N-dimethylformamide as solvent. The structure elucidation was processed through different spectral techniques including IR, 1H-NMR and EIMS. The screening of the synthesized molecules against Gram-bacterial strains, to evaluate antibacterial activity, showed them moderately good inhibitors as shown by their low MIC values. [ABSTRACT FROM AUTHOR]

The presented study comprises the synthesis of a new series of ethylated sulfonamides in which 1,4-benzodioxane moietyhas been incorporated. The reaction of 1,4-benzodioxane-6-amine (1) with ethane sulfonyl chloride (2) yielded N-(2,3-dihydrobenzo[1,4]dioxin-6-yl)ethanesulfonamide (3), which further on treatment with various alkyl/aralkyl halides, 4a-r, in N,N-dimethylformamide (DMF) and in the presence of lithium hydride (LiH) acting as a weak base and catalyst;yielded derivativesofN-alkyl/aralkyl substituted N-(2,3-dihydrobenzo[1,4]dioxin-6-yl)ethanesulfonamides (5a-r). The characterization of these derivatives was carried out by different spectroscopic techniques like infra red, proton-NMR and mass spectrometry; then screened against various enzymes i.e. acetylcholinesterase, butyrylcholinesterase, lipoxygenase and α-glucosidase enzymes and five different bacterial strains. The synthesized compounds were found to be good inhibitors of lipoxygenase but moderate inhibitors of AChE, BChE and α-glucosidase; whereas compounds 3, 5a, 5f, 5n and 5r were found good antibacterial compounds. The interaction between inhibitors and target enzymes (cholinestrases and lipoxygenase) was computationally observed which correlated with the experimental results. [ABSTRACT FROM AUTHOR]

New potent organic compounds were synthesized with an aim of good biological activities such as antibacterial and anti-enzymatic. Three series of sulfonamide derivatives were synthesized by treating N-alkyl/aryl substituted amines (2a-f) with 4-chlorobenzensulfonyl chloride (1) to yield N-alkyl/aryl-4-chlorobenzenesulfonamide(3af) that was then derivatized by gearing up with ethyl iodide (4), benzyl chloride (5) and 4-chlorobenzyl chloride (6) using sodium hydride as base to initialize the reaction in a polar aprotic solvent (DMF) to synthesize the derivatives, 7a-f, 8afand 9a-f respectively. Structure elucidation was brought about by IR, ¹H-NMR and EIMS spectra for all the synthesized molecules which were evaluated for their antibacterial activities and inhibitory potentials for certain enzymes. [ABSTRACT FROM AUTHOR]

The biological potential of N'-substituted-2-(5-(3-chlorophenyl)-l,3,4-Oxadiazol-2-ylthio)acetohydrazide (8ap) has been evaluated against bacterial strains of Gram-negative and Gram-positive bacteria. The multistep synthesis involved the conversion of 3-chlorobenzoic acid (1) to ethyl 3-chlorobenzoate (2), 3-chlorobenzohydrazide (3) 5-(3- chlorophenyl)-1,3,4-Oxadiazol-2-thiol (4), ethyl 2-(5-(3-chlorophenyl)-l,3,4-Oxadiazol-2-ylthio) acetate (5) and 2-(5- 3- chlorophenyl)-1,3,4-Oxadiazol-2-ylthio)acetohydrazide (6). The last step involved the reaction of 6 and aryl aldehydes 7a-p in methanol to synthesize the Schiff bases, 8a-p, with better yields. The structures of all the molecules were corroborated by spectral analysis. The Schiff bases were further evaluated for the antibacterial activity and found to be moderately good inhibitors of bacterial strains of Gram-bacteria. [ABSTRACT FROM AUTHOR]

A new series of N-substituted derivatives of 2-{(5-phenyl-1,3,4-Oxadiazol-2-yl)sulfanyl}acetamides was synthesized. The synthesis was carried out by converting benzoic acid (1) into ethyl benzoate (2), benzohydrazide (3) and then 5-pheny-1,3,4-Oxadiazol-2-thiol (4) step by st0ep. The target compounds 6a-p were synthesized by reaction of compound 4 with equimolar ratios of different N-alkyl/aryl substituted 2-bromoacetamide (5a-p) in the presence of DMF and sodium hydride (NaH). The spectral (EI-MS, IR, 1H-NMR) characterization of all the synthesized compounds reveal their successful synthesis. The compounds were also screened for antimicrobial & hemolytic activity and most of them were found to be active against the selected microbial species at variable extent relative to reference standards. But 6h was the most active against the selected panel of microbes. This series showed less toxicity and may be considered for further biological screening and application trial except 6m, possessing higher cytotoxicity. [ABSTRACT FROM AUTHOR]

The most emerging class among the heterocyclic compounds is 1,3,4-oxadiazoles for their diverse biological activities. In the present research work, piperonylic acid (1) was converted consecutively into corresponding ester (2), hydrazide (3) and 1,3,4-oxadiazole (4) through intermolecular cyclization. The synthesized compound 4 was subjected further to S-alkylation/aralkylation, using alkyl/aralkyl halides (5a-m) and S-substituted-1,3,4-oxadiazole derivatives were synthesized (6a-m). The structure elucidation of the synthesized molecules was processed through ¹H-NMR, IR and mass spectral data. The antibacterial activity showed these molecules moderately good inhibitors of gram-negative and gram-positive bacteria. [ABSTRACT FROM AUTHOR]

Pyrus pashia Buch. & Ham. was subjected to extraction with methanol. Methanolic extracts of fruit, bark and leaf were partitioned separately with four organic solvents in order of increasing polarity, asn-hexane, chloroform, ethyl acetate and n-butanol after dissolving in distilled water. Phytochemical screening revealed the presence of phenolics, flavonoides, alkaloids and cardiac glycosides in large amount in chloroform, ethyl acetate and n-butanol soluble fractions. The antioxidant activity of crude methanolic extracts, all the obtained fourorganic fractions and remaining aqueous fractions was evaluated by different methods such as: 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity, ferric reducing antioxidant power (FRAP) assay and total antioxidant activity by phosphomolybdenum complex method as well as determination of total phenolics. The results of antioxidant activity exhibited that chloroform soluble fraction of fruit showed the highest value of percent inhibition of DPPH (48.16± 0.21µg/ml) at the concentration of 10µg/ml. Ethyl acetate soluble fraction displayed the lowest antioxidant activity havingIC50 value of bark as (8.64±0.32µg/ml) relative to butylated hydroxytoluene (BHT), having IC50 of 12.1± 0.92µg/ml. The ethyl acetate soluble fraction of bark revealed the highest FRAPs value (174.618±0.11TE µM/ml) among all the three parts. This fraction also showed the highest value of total antioxidant activity as (1.499±0.90), determined by phosphomolybdenum complex method. Moreover, this fraction also conferred the highest phenolic content (393.19± 0.72) as compared to other studied fractions of fruit and leaf. [ABSTRACT FROM AUTHOR]

Sulfonamides aie adherent to a biologically dynamic category of compounds and are under consideration of many organic synthetic researches to synthesize pharmacologically important compounds. In this demonstrated research work, a benignant series of chlorinated sulfonamides were synthesized and screened against different enzymes. These various chlorinated sulfonamides (3a-i) were set up by pairing of different substituted anilines (2a-i) with 4- chlorobenzenesulfonyl chloride (1) under basic pH in an aqueous media. The structures of the synthesized chlorinated sulfonamides were furnished by ¹H-NMR, IR & EI-MS. The different enzymes used for the evaluation of bioactivity of all the synthesized compounds were urease, butyrylcholinesterase (BChE) and lipoxygenase (LOX). All the compounds exhibited good inhibitory activities against these enzymes but the strong activity was shown against BChE and hence can be employed for discovery o f 'lead' compounds against Alzheimer's disease (AD). [ABSTRACT FROM AUTHOR]

A new series of N-aryl/aralkyl substitued-2″-[(phenylsulfonyl)(piperidin-1-yl)amino]acetamide (7a-k) was synthesized. These derivatives were geared up by the pairing of benzenesulfonyl chloride (4) with 1-aminopiperidine (5) under dynamic pH control in aqueous media to afford parent compound N-(Piperidin-1-yl) benzenesulfonamide (6), followed by the substitution at nitrogen atom with different electrophiles N-aryl/aralkyl-substituted-2-bromoacetamides (3a-k) in the presence of sodium hydride (NaH) and N,N-Dimethylformamide (DMF) to give a new series of N-substituted derivatives of acetamide (7a-k) bearing piperidine moiety. All the synthesized compounds were confirmed on the basis of IR, EIMS and ¹H-NMR spectral data. The synthesized compounds were evaluated against acetylcholinesterase and butyrylcholinesterase (AChE and BChE) respectively and lipoxygenase (LOX) enzymes. Almost all the synthesized compounds displayed promising activity but few of them remained inactive against lipoxygenase enzymes. [ABSTRACT FROM AUTHOR]

In the present work, a series of 2-O-substituted derivatives of 1-[(3,5-dichloro-2-hydroxy phenyl) sulfonyl]piperidine (5a-j) were synthesized. These derivatives were geared up by the coupling of 3,5-dichloro-2-hydroxy benzenesullbnyl chloride (1) with piperidine (2) under dynamic pH control in aqueous media to form parent compound 1-[(3,5-dichloro-2-hydroxyphenyl)sulfonyl]piperidine (3), followed by the substitution at oxygen atom with different electrophiles (4a-j) in the presence of sodium hydride (Nail) and dimethyl formamide (DMF) to give a series of O- substituted derivatives of sulfonamides bearing piperidine nucleus 5a-j. The synthesized O-substituted sultbnamides were spectrally characterized. The bioactivity of all the synthesized compounds were evaluated against lipoxygenase (LOX), acetylcholinesterae (ACHE) and butyrylcholinesterase (BChE) enzymes and found to be having talented activity against butyrylcholinesterase enzyme. [ABSTRACT FROM AUTHOR]

A series of new N-substituted derivatives of 5-benzyl-l, 3, 4-oxadiazole-2yl-2"-sulfanyl acetamide (6a-n) were synthesized in three phases. The first phase involved the sequentially converting phenyl acetic acid into ester, hydrazide and finally cyclized in the presence of CS2 to afford 5-benzyl-1, 3, 4-oxadiazole-2-thiol. In the second phase N-substimted-2-bromoacetamides were prepared by reacting substituted amines with bromoacetyl bromide in basic media. In the third phase, 5-benzyl-l,3,4-oxadiazole-2-thiol was stirred with N-substituted-2-bromoacetamides in the presence of N,N-dimethyl formamide (DMF) and sodium hydride (Nail) to get the target compounds. Spectral techniques were used to confirm the structures of synthesized compounds. Synthesized compounds were screened against butyrylcho linesterase (BChE), acetylcholinesterase (ACHE), and lipoxygenase enzymes (LOX) and were found to be relatively more active against acetylcholinesterase. [ABSTRACT FROM AUTHOR]

In the current study, a series of 5-substituted-1,3,4-oxadiazole-2yl-N-(2-methoxy-5-chlorophenyl)-2-sulfanyl acetamide was synthesized by converting variously substituted/unsubstituted aromatic organic acids successively into the corresponding esters, hydrazides and then 5-substituted-1,3,4-oxadiazole-2-thiols. Finally the target compounds were obtained by stirring 5-substituted-1,3,4-oxadiazole-2-thiols with N-(2-methoxy-5-chlorophenyl)-2-bromoacetamide in the presence of MN-dimethyl formamide (DMF) and sodium hydride (NaH). The structures of the synthesized compounds were confirmed based on ¹H-NMR, IR and mass spectral data. The synthesized compounds were screened against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and lipoxygenase enzymes (LOX) and were found to be relatively more active against acetyl cholinesterase. [ABSTRACT FROM AUTHOR]

In the present study, a series of N-substituted derivatives of 2-phenylethylamine has been synthesized. The reaction of 2-phenylethylamine (1) with benzene sulfonyl chloride (2) yielded N-(2-phenylethyl) benzenesulfonamide (3), which further on treatment with alkyl/acyl halides (4a-i) in the presence of sodium hydride furnished into Nsubstituted sulfonamides (5a-i). These derivatives were characterized by IR, ¹H-NMR and EI-MS and then screened against acetyl cholinesterase (AChE), butyryl cholinesterase (BChE) and lipoxygenase enzyme (LOX) and were found to be potent inhibitors of butyryl cholinesterase only. [ABSTRACT FROM AUTHOR]

Methanolic extract of Cotinus coggyria Scop. was mixed in distilled water and partitioned first with the nhexane, then with chloroform, then ethyl acetate and at the end with n-butanol. The phytochemical screening of plant showed presence of the phenolics, cardiac glycosides and flavonoides in large amount in the chloroform, n-butanol and ethyl acetate soluble fraction. Antioxidant activity of these four fractions and the left behind aqueous fraction was measured by four methods such as: 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity, ferric thiocyanate assay, ferric reducing antioxidant power (FRAP) assay and total antioxidant activity. Total phenolics were also measured. Noteworthy antioxidant potential was shown by the chloroform, n-butanol and ethyl acetate soluble fraction showed. Ethyl acetate fraction showed highest % inhibition of the DPPH radical when compared with the other studied fractions i.e. 81.64 ± 1.29% inhibition of the DPPH radical at the concentration of 30 µg/ml. Its IC50 value was found to be 15.58 ± 0.09 µg/ml, comparative to the butylated hydroxytoluene (BHT), which has IC50 value 12.6 ± 0.85µg/mL. This fraction also showed the highest lipid peroxidation inhibition (61.41 ± 1.16%), as well as highest values of FRAP (697.76 ± 1.98 µg of trolox equivalents) total antioxidant activity (1.02 ± 0.09) and total phenolic contents (229.34 ± 0.57) comparative to the other studied fractions. The chloroform and n-butanol soluble fraction also showed good results for all the studied antioxidant assays. [ABSTRACT FROM AUTHOR]

Methanolic extract of Boerhavia procumbens Bank ex Roxb. was partitioned with n-hexane, chloroform, ethyl acetate and n-butanol sequentially after dissolving in distilled water. Phytochemical screening showed presence of phenolics, flavonoides and cardiac glycosides in large amount in chloroform, ethyl acetate and n-butanol soluble fraction. The antioxidant activity of all these fractions and the remaining aqueous fraction was evaluated by four methods such as: 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity, ferric reducing antioxidant power (FRAP) assay, total antioxidant activity and ferric thiocyanate assay. Total phenolics were also determined. Some fractions showed noteworthy antioxidant activity. The results of the antioxidant activity revealed that the ethyl acetate soluble fraction showed the highest value of percent inhibition of DPPH (82.54 ±0.62) at the concentration of 125 µg/ml. The IC50 of this fraction was 37.11± 0.23 µg/ml, compared with butylated hydroxytoluene (BHT), which have IC50 of 12.1± 0.92 µg/mL. It also showed the highest FRAP value (251.08 ±1.46 µg of trolox equivalents) as well as the highest value of lipid peroxidation inhibition (57.21 ± 52%), the highest total antioxidant activity (0.549 ±0.08) and also the highest total phenolic contents (77.1± 0.6) as compared to the studied fractions. Phytochemical screening showed high percentage of phenolics, flavonoides and cardiac glycosides in this fraction. [ABSTRACT FROM AUTHOR]