Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme

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dc.authoridBozbey Merde, Irem/0000-0002-9290-938X
dc.authoridTaskor Onel, Gulce/0000-0002-9375-2329
dc.contributor.authorBozbey, Irem
dc.contributor.authorOnel, Gulce Taskor
dc.contributor.authorTurkmenoglu, Burcin
dc.contributor.authorGursoy, Sule
dc.contributor.authorDilek, Esra
dc.contributor.authorErgun, Muhammed
dc.contributor.authorOzcelik, Azime Berna
dc.date.accessioned2024-10-26T18:00:34Z
dc.date.available2024-10-26T18:00:34Z
dc.date.issued2022
dc.departmentSivas Cumhuriyet Üniversitesi
dc.description.abstractAlzheimer's disease is a neurological disease characterized by the destruction of brain cells. In this disease, which causes a decrease in thought, memory and behavioral functions, the symptoms appear gradually with age. In this study, inhibition of acetylcholinesterase enzyme which is an important target in accordance with the cholinergic hypothesis, was studied. New 3(2H)pyridazinone-triazole derivatives were synthesized, confirmed by 1H-NMR, 13CNMR, HRMS analysis and their IC50 and Ki values were studied. The inhibition constants (Ki) of the compounds against the AChE enzyme ranged from 2.35 +/- 0.18 to 5.15 +/- 0.46 mu M. The compound with the best inhibitory properties was compound 6d with a Ki value of 2.35 +/- 0.18 mu M. In addition, to support the experimental data, molecular docking studies were carried out with 6b, 6d, 6e and 6f compounds with AChE crystal structure (PDB ID:4M0E).
dc.description.sponsorshipErzincan Binali Yildirim University [TSA-2020-664]; Erzincan Binali Yildirim University, Basic Sciences Application and Research Center (EBYU-EUTAM)
dc.description.sponsorshipWe thank Erzincan Binali Yildirim University (Project Number: TSA-2020-664) for their financial support. The authors would like to thank Erzincan Binali Yildirim University, Basic Sciences Application and Research Center (EBYU-EUTAM) for the Schrodinger Maestro 2021-2 program.
dc.identifier.doi10.29228/jrp.239
dc.identifier.endpage1471
dc.identifier.issn2630-6344
dc.identifier.issue5
dc.identifier.scopus2-s2.0-85137920793
dc.identifier.scopusqualityQ3
dc.identifier.startpage1461
dc.identifier.trdizinid1125969
dc.identifier.urihttps://doi.org/10.29228/jrp.239
dc.identifier.urihttps://search.trdizin.gov.tr/tr/yayin/detay/1125969
dc.identifier.urihttps://hdl.handle.net/20.500.12418/27755
dc.identifier.volume26
dc.identifier.wosWOS:000929825400035
dc.identifier.wosqualityN/A
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakTR-Dizin
dc.language.isoen
dc.publisherMarmara Univ
dc.relation.ispartofJournal of Research in Pharmacy
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectAcetylcholinesterase
dc.subjectalzheimer's disease
dc.subjectmolecular docking
dc.subjectpyridazinone
dc.subjecttriazole
dc.titleInhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme
dc.typeArticle

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