Quinazolinone-based benzenesulfonamides with low toxicity and high affinity as monoamine oxidase-A inhibitors: Synthesis, biological evaluation and induced-fit docking studies

Bioorganic Chemistry, Год журнала: 2022, Номер 124, С. 105822 - 105822

Опубликована: Апрель 22, 2022

Язык: Английский

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Exploration of Some Bis‐Sulfide and Bis‐Sulfone Derivatives as Non‐Classical Aldose Reductase İnhibitors

ChemistrySelect, Год журнала: 2023, Номер 8(5)

Опубликована: Фев. 2, 2023

Abstract Aldose reductase (AR, ALR2; EC 1.1.1.21), an enzyme that converts glucose to fructose on the polyol pathway, is important member of Aldo‐keto superfamily. ALR2 part rate‐limiting step, which associated with diabetic complications in this process, and plays a role regulating reactive oxygen species induced by growth factors cytokines. Despite fact sulfides sulfones have been discovered variety other biological functions, current study, we assessed inhibitory potential derivatives bis‐sulfide ( 5 – i ) bis‐sulfone 6 order further our interest designing discovering powerful inhibitors. The results investigations showed all exhibit activity against ALR2, K I values ranging from 0.53±0.03 4.20±0.06 μM. Among these agents, 2,6‐bis((4‐chlorophenyl)(phenylthio)methyl)cyclohexan‐1‐one h ), 2,6‐bis((3‐nitrophenyl)(phenylthio)methyl)cyclohexan‐1‐one c 2,6‐bis((3‐chlorophenyl)(phenylthio)methyl)cyclohexan‐1‐one g exhibited prominent constants μM, 0.65±0.04 0.71±0.05 respectively, were found be more potent than epalrestat =0.79±0.01 μM) currently, only inhibitor (ALR2I) utilized treatment. Additionally, silico molecular docking experiments carried out explain how bis‐sulfides bis‐sulfones interacted target ALR2′s binding site. According ADME‐Tox compounds are predicted ALR2Is appropriate drug‐like characteristics. study‘s findings could exploited create innovative therapeutics prevent diabetes complications.

Язык: Английский

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Novel sulfonamide derivatives as multitarget antidiabetic agents: design, synthesis, and biological evaluation

RSC Advances, Год журнала: 2024, Номер 14(11), С. 7664 - 7675

Опубликована: Янв. 1, 2024

A series of new sulfonamide derivatives connected through an imine linker to five or seven membered heterocycles were designed and synthesized.

Язык: Английский

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Calcium Channel Blockers: The Effect of Glutathione S‐Transferase Enzyme Activity and Molecular Docking Studies

ChemistrySelect, Год журнала: 2021, Номер 6(40), С. 11137 - 11143

Опубликована: Окт. 26, 2021

Abstract Recently, as a drug target in cancer treatment, the superfamily of glutathione S‐transferase (GSTs, EC 2.5.1.18) have been invited considerable interest by scientists. In particular, they are overexpressed many human cell lines, GSTs can catalyze conjugation cellular nucleophile (GSH) with wide range electrophilic carcinogens toxins and drugs, meanwhile producing oxidative stress. For this purpose, GST was purified GSH‐agarose affinity chromatography, some calcium channel blockers (CCBs), such amlodipine, cinnarizine, isradipine, nifedipine, nilvadipine, were assessed for their inhibitory actions against GST. The CCBs demonstrated micromolar levels activity towards ( K I s spanning within 98.84±0.53 μM–502.70±2.53 μM range). best observed isradipine. Additionally, molecular docking study performed competitive inhibitor nilvadipine on to describe possible interaction active site confirm activity.

Язык: Английский

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PEPPSI type Pd(II)NHC complexes bearing chloro-/fluorobenzyl group: Synthesis, characterization, crystal structures, α-glycosidase and acetylcholinesterase inhibitory properties

Polyhedron, Год журнала: 2021, Номер 198, С. 115060 - 115060

Опубликована: Янв. 27, 2021

Язык: Английский

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