Design, synthesis, and molecular modeling of new 3(2H)-pyridazinone derivatives as acetylcholinesterase/butyrylcholinesterase inhibitors

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dc.authoridSARI, SUAT/0000-0002-8248-4218
dc.authoridSenol Deniz, F. Sezer/0000-0002-5850-9841
dc.authoridSARI, SUAT/0000-0002-8248-4218
dc.authoridOzdemir, Zenyep/0000-0003-4559-2305
dc.authoridKarakurt, Arzu/0000-0003-2209-0871
dc.authorwosidSARI, SUAT/A-5249-2017
dc.authorwosidSenol Deniz, F. Sezer/AAG-5636-2019
dc.authorwosidSARI, SUAT/JCD-8070-2023
dc.authorwosidOzdemir, Zenyep/AAJ-6384-2020
dc.authorwosidKarakurt, Arzu/ABH-9340-2020
dc.contributor.authorOzdemir, Zeynep
dc.contributor.authorYilmaz, Hayriye
dc.contributor.authorSari, Suat
dc.contributor.authorKarakurt, Arzu
dc.contributor.authorSenol, Fatma Sezer
dc.contributor.authorUysal, Mehtap
dc.date.accessioned2024-08-04T20:43:11Z
dc.date.available2024-08-04T20:43:11Z
dc.date.issued2017
dc.departmentİnönü Üniversitesien_US
dc.description.abstractInhibition of cholinesterases is an effective method to curb Alzheimer's disease, a progressive and fatal neurological disorder. A series of 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(p-substituted benzalhidrazone) derivatives were designed, synthesized, and their inhibitory effects on acetylcholinesterase and butyrylcholinesterase were evaluated in pursuit of potent dual inhibitors. We obtained our compounds by the reaction of various substituted/nonsubstituted benzaldehydes with 6-[4-(3,4-dichlorophenyl)piperazine-1-yl]-3(2H)-pyridazinone-2-yl acetohydrazide and determined their anticholinesterase activities according to the Ellman's method. 5f and 5i showed 75.52 and 71.72% acetylcholinesterase inhibition at 100 A mu g/ml, respectively. 5h and 5f, on the other hand, were the best butyrylcholinesterase inhibitors with 67.16 and 62.03% inhibition at the same concentration, respectively. 5f emerged as a potent dual cholinesterase inhibitor. Through molecular docking studies we predicted the inhibition mechanism of 5f for both enzymes in comparison with our previous derivatives, which differ in inhibition potency, and tried to get insights into the factors that affect receptor affinity in molecular level.en_US
dc.description.sponsorshipResearch Foundation of Inonu University [2013/94]en_US
dc.description.sponsorshipThis study was funded by the Research Foundation of Inonu University (2013/94).en_US
dc.identifier.doi10.1007/s00044-017-1930-x
dc.identifier.endpage2308en_US
dc.identifier.issn1054-2523
dc.identifier.issn1554-8120
dc.identifier.issue10en_US
dc.identifier.scopus2-s2.0-85020060248en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.startpage2293en_US
dc.identifier.urihttps://doi.org/10.1007/s00044-017-1930-x
dc.identifier.urihttps://hdl.handle.net/11616/97834
dc.identifier.volume26en_US
dc.identifier.wosWOS:000412416600007en_US
dc.identifier.wosqualityQ4en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherSpringer Birkhauseren_US
dc.relation.ispartofMedicinal Chemistry Researchen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectAChE inhibitoryen_US
dc.subjectBChE inhibitoryen_US
dc.subject3(2H)-Pyridazinoneen_US
dc.subjectBenzalhydrazoneen_US
dc.subjectMolecular dockingen_US
dc.titleDesign, synthesis, and molecular modeling of new 3(2H)-pyridazinone derivatives as acetylcholinesterase/butyrylcholinesterase inhibitorsen_US
dc.typeArticleen_US

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