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Benzenesulfonamide derivatives as potent acetylcholinesterase, α-glycosidase, and glutathione S-transferase inhibitors: biological evaluation and molecular docking studiesTaslimi, ParhamIşık, MesutTürkan, FikretDurgun, MustafaTürkeş, CüneytGülçin, İlhamiBeydemir, Şükrüacetylcholinesteraseglutathione S-transferasemolecular dockingsulfonamide derivativesα-GlycosidaseCholinesterase InhibitorsGlutathione TransferaseGlycoside HydrolasesMolecular Docking SimulationStructure-Activity RelationshipSulfonamidesalpha glycosidasebenzenesulfonamide derivativeglycosidasemethanolsodium borohydrideunclassified drugbenzenesulfonamidecholinesterase inhibitorsulfonamideArticleconcentration responsecrystal structuredrug activitydrug bindingdrug structureenzyme inhibitionpriority journalreceptor bindingstructure activity relationSulfonamide derivatives exhibit a wide biological activity and can function as potential medical molecules in the development of a drug. Studies have reported that the compounds have an effect on many enzymes. In this study, the derivatives of amine sulfonamide (1i-11i) were prepared with reduced imine compounds (1-11) with NaBH4 in methanol. The synthesized compounds were fully characterized by spectral data and analytical. The effect of the synthesized derivatives on acetylcholinesterase (AChE), glutathione S-transferase (GST) and α-glycosidase (α-GLY) enzymes were determined. For the AChE and α-GLY, the most powerful inhibition was observed on 10 and 10i series with K I value in the range 2.26 ± 0.45–3.57 ± 0.97 and 95.73 ± 13.67–102.45 ± 11.72 µM, respectively. K I values of the series for GST were found in the range of 22.76 ± 1.23–49.29 ± 4.49. Finally, the compounds have a stronger inhibitor in lower concentrations by the attachment of functional electronegative groups such as two halogens (-Br and -CI), -OH to the benzene ring and -SO2NH2. The crystal structures of AChE, α-GLY, and GST in complex with selected derivatives 4 and 10 show the importance of the functional moieties in the binding modes within the receptors. Communicated by Ramaswamy H. Sarma. © 2020, © 2020 Informa UK Limited, trading as Taylor & Francis Group.Taylor and Francis Ltd.2020Articlehttps://rdlopen.rawdatalibrary.net/r/ebyu/13903https://doi.org/10.1080/07391102.2020.17904220739-1102enJournal of Biomolecular Structure and Dynamicsinfo:eu-repo/semantics/openAccessinfo:eu-repo/semantics/articlehttps://ebyu-rdlopen.rawdatalibrary.net/tr/items/ebyu/13903