Inhibition of Cholinesterases by Benzothiazolone Derivatives

Basit Öğe Kaydı
dc.authoridOnkol, Tijen/0000-0003-3973-5728
dc.authoridOzdemir, Zenyep/0000-0003-4559-2305
dc.authoridSARI, SUAT/0000-0002-8248-4218
dc.authoridSARI, SUAT/0000-0002-8248-4218
dc.authoridalagoz, mehmet abdullah/0000-0001-5190-7196
dc.authoridKim, Hoon/0000-0002-7203-3712
dc.authoridARSLAN, Gulnur/0000-0001-9054-7437
dc.authorwosidOnkol, Tijen/AAA-2377-2021
dc.authorwosidMathew, Bijo/HTS-6728-2023
dc.authorwosidOzdemir, Zenyep/AAJ-6384-2020
dc.authorwosidSARI, SUAT/JCD-8070-2023
dc.authorwosidSARI, SUAT/A-5249-2017
dc.authorwosidalagoz, mehmet abdullah/W-7847-2018
dc.authorwosidNicolotti, Orazio/F-3209-2012
dc.contributor.authorAlagoz, Mehmet Abdullah
dc.contributor.authorKim, Seong-Min
dc.contributor.authorOh, Jong Min
dc.contributor.authorArslan, Gulnur
dc.contributor.authorOzdemir, Zeynep
dc.contributor.authorSari, Suat
dc.contributor.authorOzcelik, Azime Berna
dc.date.accessioned2024-08-04T20:53:02Z
dc.date.available2024-08-04T20:53:02Z
dc.date.issued2022
dc.departmentİnönü Üniversitesien_US
dc.description.abstractThirteen benzothiazolone derivatives (M1-M13) were synthesized and evaluated for their inhibitory activity against cholinesterases (ChEs) and monoamine oxidases (MAOs). All the compounds inhibited ChEs more effectively than MAOs. In addition, most of the compounds showed higher inhibitory activities against butyrylcholinesterase (BChE) than acetylcholinesterase (AChE). Compound M13 most potently inhibited BChE with an IC50 value of 1.21 mu M, followed by M2 (IC50 = 1.38 mu M). Compound M2 had a higher selectivity index (SI) value for BChE over AChE (28.99) than M13 (4.16). The 6-methoxy indole group of M13 was expected to have a greater effect on BChE inhibitory activity than the other groups. Kinetics and reversibility tests showed that M13 was a reversible noncompetitive BChE inhibitor with a K-i value of 1.14 +/- 0.21 mu M. In a docking simulation, M13 is predicted to form a hydrogen bond with the backbone carbonyl group of Ser287 of BChE through its methoxy indole moiety and pi-pi interactions between its benzothiazolone group and the side chain of Trp82 with the five-membered pyrrole ring and with the six-membered benzene ring. From these results, it is suggested that M13 is a BChE inhibitor and a potential candidate agent for the treatment of Alzheimer's disease.en_US
dc.description.sponsorshipResearch Promotion Program of SCNUen_US
dc.description.sponsorshipThis work was supported by a Research Promotion Program of SCNU (To H.K.).en_US
dc.identifier.doi10.3390/pr10091872
dc.identifier.issn2227-9717
dc.identifier.issue9en_US
dc.identifier.scopus2-s2.0-85138694760en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.3390/pr10091872
dc.identifier.urihttps://hdl.handle.net/11616/100910
dc.identifier.volume10en_US
dc.identifier.wosWOS:000856915700001en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherMdpien_US
dc.relation.ispartofProcessesen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectbenzothiazoloneen_US
dc.subjectcholinesterase inhibitoren_US
dc.subjectkineticsen_US
dc.subjectdocking analysisen_US
dc.titleInhibition of Cholinesterases by Benzothiazolone Derivativesen_US
dc.typeArticleen_US

Dosyalar

Koleksiyon

WoS İndeksli Yayınlar Koleksiyonu
Scopus İndeksli Yayınlar Koleksiyonu