Vinyl functionalized 5,6-dimethylbenzimidazolium salts: Synthesis and biological activities

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dc.authoridGurbuz, Nevin/0000-0003-3201-3597
dc.authoridGulcin, ilhami/0000-0001-5993-1668
dc.authoridOzdemir, Ismail/0000-0001-6325-0216
dc.authorwosidOZDEMIR, ISMAIL/KVY-3420-2024
dc.authorwosidGurbuz, Nevin/A-3069-2016
dc.authorwosidGulcin, ilhami/F-1428-2014
dc.contributor.authorKaraca, Emine O.
dc.contributor.authorBingol, Zeynebe
dc.contributor.authorGurbuz, Nevin
dc.contributor.authorOzdemir, Ismail
dc.contributor.authorGulcin, Ilhami
dc.date.accessioned2024-08-04T20:53:12Z
dc.date.available2024-08-04T20:53:12Z
dc.date.issued2023
dc.departmentİnönü Üniversitesien_US
dc.description.abstractA series of vinyl functionalized 5,6-dimethylbenzimidazolium salts are synthesized. All compounds were fully characterized by elemental analyses, MS, H-1-NMR, C-13-NMR, and IR spectroscopy techniques. Enzyme inhibition is a very active area of research in drug design and development. In this study, the synthesized novel benzimidazolium salts were evaluated toward the human erythrocyte carbonic anhydrase I (hCA I), and II (hCA II) isoenzymes, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. They demonstrated highly potent inhibition ability against hCA I with K-i values of 484.8 +/- 62.6-1389.7 +/- 243.2 nM, hCA II with K-i values of 298.9 +/- 55.7-926.1 +/- 330.0 nM, alpha-glycosidase with K-i values of 170.3 +/- 27-760.1 +/- 269 mu M, AChE with K-i values of 27.1 +/- 3-77.6 +/- 1.7 nM, and BChE with K-i values of 21.0 +/- 5-61.3 +/- 15 nM. As a result, novel vinyl functionalized 5,6-dimethylbenzimidazolium salts (1a-g) exhibited effective inhibition profiles toward studied metabolic enzymes. Therefore, we believe that these results may contribute to the development of new drugs particularly to treat some global disorders including glaucoma, Alzheimer's disease, and diabetes.en_US
dc.description.sponsorshipInoenue University Research Fund [IUE-BAP: FBG-2021-2562, IUE-BAP: FCD-2019-1985]en_US
dc.description.sponsorshipInoenue University Research Fund, Grant/Award Numbers: IUE-BAP: FBG-2021-2562, IUE-BAP: FCD-2019-1985en_US
dc.identifier.doi10.1002/jbt.23255
dc.identifier.issn1095-6670
dc.identifier.issn1099-0461
dc.identifier.issue2en_US
dc.identifier.pmid36424355en_US
dc.identifier.scopus2-s2.0-85142625661en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1002/jbt.23255
dc.identifier.urihttps://hdl.handle.net/11616/101016
dc.identifier.volume37en_US
dc.identifier.wosWOS:000890888100001en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherWileyen_US
dc.relation.ispartofJournal of Biochemical and Molecular Toxicologyen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subject5,6-dimethylbenzimidazolium saltsen_US
dc.subjectacetylcholinesteraseen_US
dc.subjectbutyrylcholinesteraseen_US
dc.subjectcarbonic anhydraseen_US
dc.subjectenzyme inhibitionen_US
dc.subjectalpha-glycosidaseen_US
dc.titleVinyl functionalized 5,6-dimethylbenzimidazolium salts: Synthesis and biological activitiesen_US
dc.typeArticleen_US

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