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Your search keyword '"Mohammed Samim"' showing total 4 results
Start Over Author "Mohammed Samim" Journal journal of enzyme inhibition and medicinal chemistry
4 results on '"Mohammed Samim"'

1. Synthesis, biological evaluation and theoretical studies of (E)-1-(4-sulfamoyl-phenylethyl)-3-arylidene-5-aryl-1H-pyrrol-2(3H)-ones as human carbonic anhydrase inhibitors

Author

Farhat Ramzan, Syed Ayaz Nabi, Mehak Saba Lone, Alessandro Bonardi, Aabid Hamid, Sameena Bano, Kalicharan Sharma, Syed Shafi, Mohammed Samim, Kalim Javed, and Claudiu T. Supuran

Subjects
Human carbonic anhydrase, benzenesulphonamide, pyrrolone, anticancer drugs, enzyme inhibitors, Therapeutics. Pharmacology, RM1-950
Abstract

A series of 20 newly designed (E)-1-(4-sulphamoylphenylethyl)-3-arylidene-5-aryl-1H-pyrrol-2(3H)-ones was synthesised and assessed as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors towards four human isoforms of pharmaceutical interest, that is, hCA I, II, IX and XII. The compounds displayed low to high nanomolar potency against all the isoforms. Introducing strong electron withdrawing groups at the para position of the arylidene ring increased the binding affinity to the enzyme. All compounds showed acceptable pharmacokinetic range and physicochemical characteristics as determined by computational ADMET analysis. Density Functional Theory (DFT) calculations of 3n were carried to gain understanding on the stability of the E and Z isomers. The energy values clearly indicate the stability of E isomer over Z isomer by −8.2 kJ mol−1. Our findings indicate that these molecules are useful as leads for discovering new CA inhibitors.

Published
2023
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2. Design and synthesis of pyridazinone-substituted benzenesulphonylurea derivatives as anti-hyperglycaemic agents and inhibitors of aldose reductase – an enzyme embroiled in diabetic complications

Author

Ameer Ismael, Syed Ovais, Alhamza Dheyaa, G. Bhanuprakash Reddy, Surender Singh, Syed Shafi, Mohammed Samim, Kalicharan Sharma, Ayad Ahmed, Kalim Javed, Pooja Rathore, H. Pushpalatha, Raed Yaseen, and Mymoona Akthar

Subjects
Male, 0301 basic medicine, medicine.drug_class, Pharmacology, Diabetes Complications, 03 medical and health sciences, chemistry.chemical_compound, Aldehyde Reductase, Lens, Crystalline, Drug Discovery, medicine, Animals, Hypoglycemic Agents, Gliclazide, Rats, Wistar, IC50, Aldose reductase, Spectrum Analysis, Area under the curve, General Medicine, Sulfonylurea, Rats, Pyridazines, Sulfonylurea Compounds, 030104 developmental biology, chemistry, Biochemistry, Docking (molecular), Area Under Curve, Drug Design, Female, Quercetin, medicine.drug
Abstract

Thirty new aryl-pyridazinone-substituted benzenesulphonylurea derivatives (I-XXX) were synthesized and evaluated for their anti-hyperglycaemic activity in glucose-fed hyperglycaemic normal rats. Twenty-three compounds (III-XI, XIV-XVII, XIX-XXIV, XXVI and XXVIII-XXX) showed more or comparable area under the curve (AUC) reduction percentage (ranging from 21.9% to 35.5%) as compared to the standard drug gliclazide (22.0%). On the basis of docking results, 18 compounds were screened for their in vitro ability to inhibit rat lens aldose reductase. Ten compounds (III-VI, XII, XVI-XVIII, XXI and XXVII) showed ARI activity with IC50 ranging from 34 to 242 μM. Out of these, two compounds IV and V showed best ARI activity which is comparable with that of quercetin. As a result, two compounds (IV and V) possessing significant dual action (anti-hyperglycaemic and aldose reductase inhibition) were identified and may be used as lead compounds for developing new drugs.

Published
2016

3. Synthesis and blood glucose lowering activity of some novel benzenesulfonylthiourea derivatives substituted with 4-aryl-1-oxophthalazin-2(1H)yl-ones

Author

Mohammed Samim, Rafia Bashir, Kalim Javed, Shafiya Yaseen, Pooja Rathore, and Syed Ovais

Subjects
Blood Glucose, Male, Stereochemistry, Rat model, Medicinal chemistry, Structure-Activity Relationship, chemistry.chemical_compound, Isothiocyanates, Drug Discovery, Acetone, Animals, Hypoglycemic Agents, Rats, Wistar, Pharmacology, Glucose lowering, Aryl, Benzenesulfonates, Thiourea, General Medicine, Rats, Glucose, chemistry, Elemental analysis, Drug Design, Hyperglycemia, Isothiocyanate, Anhydrous, Proton NMR, Phthalazines, Female
Abstract

Some new benzenesulfonylthiourea derivatives substituted with phthalazones (2a–q) were synthesized by refluxing the appropriate 4-aryl-1-oxophthalazin-2(1H)yl benzenesulfonamides with isothiocyanate in dry acetone over anhydrous K2CO3. All the synthesized compounds were characterized on the basis of IR, 1H NMR, MS data and elemental analysis. These synthesized compounds (2a–q) at the dose of 20 mg/kg were tested for antihyperglycemic activity in the glucose-fed hyperglycemic normal rat model and among these compounds 2f and 2m showed modest antihyperglycemic activity.

Published
2013

4. Synthesis and anti-inflammatory activity of celecoxib like compounds

Author

Syed Ovais, Vinod Nair, Rafia Bashir, Mohammed Samim, Surender Singh, Kalim Javed, Pooja Rathore, and Shafiya Yaseen

Subjects
medicine.drug_class, Analgesic, Antineoplastic Agents, Pyrazoline, Pharmacology, Carrageenan, Nitric Oxide, Anti-inflammatory, Structure-Activity Relationship, chemistry.chemical_compound, Drug Discovery, medicine, Animals, Edema, Humans, Cell Proliferation, Sulfonamides, Dose-Response Relationship, Drug, Molecular Structure, Tumor Necrosis Factor-alpha, Melanoma, Anti-Inflammatory Agents, Non-Steroidal, General Medicine, Reference drug, medicine.disease, Rats, chemistry, Celecoxib, Cell culture, Prostaglandins, Pyrazoles, Drug Screening Assays, Antitumor, medicine.drug
Abstract

Nine novel 4-[3-(4-Dimethylamino-phenyl)-5-aryl-4,5-dihydro-pyrazol-1-yl]-benzenesulfonamides (2a-i) were synthesized and evaluated for their anti-inflammatory and antiproliferative activities. These compounds (2a-i) showed moderate to strong anti-inflammatory activity in carrageenan rat paw oedema test. Compounds 2b, 2d and 2g showing comparable anti-inflammatory activity to that of reference drug celecoxib were evaluated for their ulcerogenic and analgesic activities. The effect of 2b, 2d and 2g on the content of NO, TNF-α and PGE2 in exudates from rat paw stimulated by carrageenan was also evaluated. The compound 2c showed considerable antitumor activities against all 60 human tumor cell lines with effective GI50 (MG-MID) value of 3.63 µM. It exhibited maximum activity against melanoma (LOX IMVI and SK-MEL-5) cancer cell lines with GI50 value less than 2 μM.

Published
2012

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