Synthesis and evaluation of novel xanthene-based thiazoles as potential antidiabetic agents

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dc.authoridParham Taslimi / 0000-0002-3171-0633en_US
dc.authorscopusidParham Taslimi / 56658628800en_US
dc.authorwosidParham Taslimi / AAL-2788-2020en_US
dc.contributor.authorNaseem, Saira
dc.contributor.authorShafiq, Zahid
dc.contributor.authorTaslimi, Parham
dc.contributor.authorHussain, Saghir
dc.contributor.authorTaşkın Tok, Tuğba
dc.contributor.authorKısa, Dursun
dc.contributor.authorSaeed, Aamer
dc.contributor.authorTemirak, Ahmed
dc.contributor.authorTahir, Muhammad N.
dc.contributor.authorRauf, Khawar
dc.contributor.authorEl-Gokha, Ahmed
dc.date.accessioned2022-11-11T08:19:43Z
dc.date.available2022-11-11T08:19:43Z
dc.date.issued2022en_US
dc.departmentİstinye Üniversitesi, Mühendislik ve Doğa Bilimleri Fakültesi, Biyomedikal Mühendisliği Bölümüen_US
dc.description.abstractA series of xanthene-based thiazoles was synthesized and characterized by different scpectroscopic methods, i.e. Proton nuclear magnetic resonance (H-1 NMR), carbon nuclear magnetic resonance (C-13 NMR), infrared spectroscopy, carbon hydrogen nitrogen analysis, and X-ray crystallography. The inhibition potencies of 18 newly synthesized thiazole derivatives were investigated on the activities of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), alpha-amylase (alpha-Amy), and alpha-glycosidase (alpha-Gly) enzymes in accordance with their antidiabetic and anticholinesterase ability. The synthesized compounds have the highest inhibition potential against the enzymes at low nanomolar concentrations. Among the 18 newly synthesized molecules, 3b and 3p were superior to the known commercial inhibitors of the enzymes and have a much more effective inhibitory potential, with IC50: 2.37 and 1.07 nM for AChE, 0.98 and 0.59 nM for BChE, 56.47 and 61.34 nM for alpha-Gly, and 152.48 and 124.84 nM for alpha-Amy, respectively. Finally, the optimized 18 compounds were subjected to molecular docking to describe the interaction between thiazole derivatives and AChE, BChE, alpha-Amy, and alpha-Gly enzymes in which important interactions were monitored with amino acid residues of each target enzyme.en_US
dc.identifier.citationNaseem, S., Shafiq, Z., Taslimi, P., Hussain, S., Taskin‐Tok, T., Kisa, D., ... & El‐Gokha, A. (2022). Synthesis and evaluation of novel xanthene‐based thiazoles as potential antidiabetic agents. Archiv der Pharmazie, e2200356.en_US
dc.identifier.doi10.1002/ardp.202200356en_US
dc.identifier.scopus2-s2.0-85139966884en_US
dc.identifier.scopusqualityN/Aen_US
dc.identifier.urihttps://doi.org/10.1002/ardp.202200356
dc.identifier.urihttps://hdl.handle.net/20.500.12713/3331
dc.identifier.wosWOS:000865845500001en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.institutionauthorTaslimi, Parham
dc.language.isoenen_US
dc.publisherWILEY-V C H VERLAG GMBHen_US
dc.relation.ispartofARCHIV DER PHARMAZIEen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectAlpha-amylaseen_US
dc.subjectAlpha-glycosidaseen_US
dc.subjectCholinesteraseen_US
dc.subjectMolecular Dockingen_US
dc.subjectThiazolineen_US
dc.subjectXantheneen_US
dc.titleSynthesis and evaluation of novel xanthene-based thiazoles as potential antidiabetic agentsen_US
dc.typeArticleen_US

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