Cytotoxic effect, enzyme inhibition, and in silico studies of some novel N-substituted sulfonyl amides incorporating 1,3,4-oxadiazol structural motif

Molecular Diversity, Год журнала: 2022, Номер 26(5), С. 2825 - 2845

Опубликована: Апрель 9, 2022

Язык: Английский

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A review on ‘sulfonamides’: their chemistry and pharmacological potentials for designing therapeutic drugs in medical science

Journal of Coordination Chemistry, Год журнала: 2023, Номер 76(5-6), С. 546 - 580

Опубликована: Март 19, 2023

The discovery of new chemical entities having enhanced bioactivities and improved functionalities to overcome the prevailing antibiotic resistance emerging diseases has evolved as one most needed research areas in pharmaceutical field. Intensive been done on metal-based drugs a result, metal complexes various Schiff bases are acknowledged potential area bioinorganic chemistry account their promising applicable uses several fields science. base sulfonamides versatile pharmacophores forming stable compounds by coordinating with metals oxidation states. As therapeutic candidates, they have actively used many applications including antifungal, analgesic, anti-inflammatory, antiviral, antitumor, antibacterial more. There worldwide risk drug medical field pathogenic microbes capable deactivating substances. This review summarizes developments that taken place from 2008 2022 activities derived compounds.

Язык: Английский

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Design, synthesis, characterization, in vitro and in silico evaluation of novel imidazo[2,1-b][1,3,4]thiadiazoles as highly potent acetylcholinesterase and non-classical carbonic anhydrase inhibitors

Bioorganic Chemistry, Год журнала: 2021, Номер 113, С. 105009 - 105009

Опубликована: Май 23, 2021

Язык: Английский

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Thiazolyl-pyrazoline derivatives: In vitro and in silico evaluation as potential acetylcholinesterase and carbonic anhydrase inhibitors

International Journal of Biological Macromolecules, Год журнала: 2020, Номер 163, С. 1970 - 1988

Опубликована: Сен. 13, 2020

Язык: Английский

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Synthesis, Characterization, and Inhibition Study of Novel Substituted Phenylureido Sulfaguanidine Derivatives as α‐Glycosidase and Cholinesterase Inhibitors

Chemistry & Biodiversity, Год журнала: 2021, Номер 18(4)

Опубликована: Фев. 23, 2021

Abstract A series of six N ‐carbamimidoyl‐4‐(3‐substituted phenylureido)benzenesulfonamide derivatives were synthesized by reaction sulfaguanidine with aromatic isocyanates. In vitro and in silico inhibitory effects the novel ureido‐substituted investigated spectrophotometric methods for α‐glycosidase (α‐GLY), acetylcholinesterase (AChE), butyrylcholinesterase (BChE) enzymes associated diabetes mellitus (DM) Alzheimer's disease (AD). ‐Carbamimidoyl‐4‐{[(3,4‐dichlorophenyl)carbamoyl]amino}benzene‐1‐sulfonamide ( 2f ) showed AChE BChE effects, K I values 515.98±45.03 nM 598.47±59.18 nM, respectively, while ‐carbamimidoyl‐4‐{[(3‐chlorophenyl)carbamoyl]amino}benzene‐1‐sulfonamide 2e strong α‐GLY effect, 103.94±13.06 nM. The antidiabetic compounds are higher than their anti‐Alzheimer's because inhibition effect on diabetic enzyme is greater esterase enzymes. Indeed, metabolic important treatment DM AD.

Язык: Английский

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Novel metabolic enzyme inhibitors designed through the molecular hybridization of thiazole and pyrazoline scaffolds

Archiv der Pharmazie, Год журнала: 2021, Номер 354(12)

Опубликована: Сен. 27, 2021

New hybrid thiazolyl-pyrazoline derivatives (4a-k) were obtained through a facile and versatile synthetic procedure, their inhibitory effects on the human carbonic anhydrase (hCA) isoforms I II as well acetylcholinesterase (AChE) determined. All new thiazolyl-pyrazolines showed activity at nanomolar levels hCA I, II, AChE inhibitors, with KI values in range of 13.35-63.79, 7.01-115.80, 17.89-48.05 nM, respectively. 1-[4-(4-Cyanophenyl)thiazol-2-yl]-3-(4-piperidinophenyl)-5-(4-fluorophenyl)-2-pyrazoline (4f) 1-(4-phenylthiazol-2-yl)-3-(4-piperidinophenyl)-5-(4-fluorophenyl)-2-pyrazoline (4a) against hCAs 1-[4-(4-chlorophenyl)thiazol-2-yl]-3-(4-piperidinophenyl)-5-(4-fluorophenyl)-2-pyrazoline (4d) 1-[4-(4-nitrophenyl)thiazol-2-yl]-3-(4-piperidinophenyl)-5-(4-fluorophenyl)-2-pyrazoline (4b) identified highly potent superior to standard drugs, acetazolamide tacrine, Compounds 4a-k also evaluated for cytotoxic L929 mouse fibroblast (normal) cell line. Moreover, comprehensive ligand-receptor interaction prediction was performed using ADME-Tox, Glide XP, MM-GBSA modules Schrödinger Small-Molecule Drug Discovery Suite elucidate potential binding modes inhibitors these metabolic enzymes.

Язык: Английский

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A new series of 2,4-thiazolidinediones endowed with potent aldose reductase inhibitory activity

Open Chemistry, Год журнала: 2021, Номер 19(1), С. 347 - 357

Опубликована: Янв. 1, 2021

Abstract In an effort to identify potent aldose reductase (AR) inhibitors, 5-(arylidene)thiazolidine-2,4-diones ( 1 – 8 ), which were prepared by the solvent-free reaction of 2,4-thiazolidinedione with aromatic aldehydes in presence urea, examined for their vitro AR inhibitory activities and cytotoxicity. 5-(2-Hydroxy-3-methylbenzylidene)thiazolidine-2,4-dione 3 ) was most inhibitor this series, exerting uncompetitive inhibition a K i value 0.445 ± 0.013 µM. The IC 50 compound L929 mouse fibroblast cells determined as 8.9 0.66 µM, pointing out its safety inhibitor. Molecular docking studies suggested that exhibited good affinity binding site (PDB ID: 4JIR). Based upon silico absorption, distribution, metabolism, excretion data, is predicted have favorable pharmacokinetic features. Taking into account stands potential orally bioavailable management diabetic complications well nondiabetic diseases.

Язык: Английский

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Biological effects of bis-hydrazone compounds bearing isovanillin moiety on the aldose reductase

Bioorganic Chemistry, Год журнала: 2021, Номер 117, С. 105473 - 105473

Опубликована: Ноя. 8, 2021

Язык: Английский

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Synthesis and characterization of novel acyl hydrazones derived from vanillin as potential aldose reductase inhibitors

Molecular Diversity, Год журнала: 2022, Номер 27(4), С. 1713 - 1733

Опубликована: Сен. 14, 2022

Язык: Английский

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Novel bis-ureido-substituted sulfaguanidines and sulfisoxazoles as carbonic anhydrase and acetylcholinesterase inhibitors

Molecular Diversity, Год журнала: 2022, Номер 27(4), С. 1735 - 1749

Опубликована: Сен. 22, 2022

Язык: Английский

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