Synthesis, characterization, inhibition effects, and molecular docking studies as acetylcholinesterase, α-glycosidase, and carbonic anhydrase inhibitors of novel benzenesulfonamides incorporating 1,3,5-triazine structural motifs

Bioorganic Chemistry, Год журнала: 2020, Номер 100, С. 103897 - 103897

Опубликована: Май 4, 2020

Язык: Английский

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Exploration of 1,2,3-triazole linked benzenesulfonamide derivatives as isoform selective inhibitors of human carbonic anhydrase

Bioorganic & Medicinal Chemistry, Год журнала: 2022, Номер 77, С. 117111 - 117111

Опубликована: Ноя. 29, 2022

Язык: Английский

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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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Design, synthesis, biological evaluation and molecular docking studies of novel 1H-1,2,3-Triazole derivatives as potent inhibitors of carbonic anhydrase, acetylcholinesterase and aldose reductase

Journal of Molecular Structure, Год журнала: 2022, Номер 1257, С. 132613 - 132613

Опубликована: Фев. 10, 2022

Язык: Английский

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Discovery of novel benzenesulfonamides incorporating 1,2,3-triazole scaffold as carbonic anhydrase I, II, IX, and XII inhibitors

International Journal of Biological Macromolecules, Год журнала: 2023, Номер 239, С. 124232 - 124232

Опубликована: Март 29, 2023

Язык: Английский

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Novel beta-lactam substituted benzenesulfonamides: in vitro enzyme inhibition, cytotoxic activity and in silico interactions

Journal of Biomolecular Structure and Dynamics, Год журнала: 2023, Номер 42(12), С. 6359 - 6377

Опубликована: Авг. 4, 2023

In this study, a library of twelve beta-lactam-substituted benzenesulfonamides (

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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Benzenesulfonamide derivatives as potent acetylcholinesterase, α-glycosidase, and glutathione S-transferase inhibitors: biological evaluation and molecular docking studies

Journal of Biomolecular Structure and Dynamics, Год журнала: 2020, Номер 39(15), С. 5449 - 5460

Опубликована: Июль 21, 2020

Sulfonamide derivatives exhibit a wide biological activity and can function as potential medical molecules in the development of drug. Studies have reported that compounds an effect on many enzymes. In this study, amine sulfonamide (1i-11i) were prepared with reduced imine (1-11) NaBH4 methanol. The synthesized fully characterized by spectral data analytical. acetylcholinesterase (AChE), glutathione S-transferase (GST) α-glycosidase (α-GLY) enzymes determined. For AChE α-GLY, most powerful inhibition was observed 10 10i series KI value range 2.26 ± 0.45–3.57 0.97 95.73 13.67–102.45 11.72 µM, respectively. values for GST found 22.76 1.23–49.29 4.49. Finally, stronger inhibitor lower concentrations attachment functional electronegative groups such two halogens (-Br -CI), -OH to benzene ring -SO2NH2. crystal structures AChE, complex selected 4 show importance moieties binding modes within receptors.Communicated Ramaswamy H. Sarma

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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