A Series of New Hydrazone Derivatives: Synthesis, Molecular Docking and Anticholinesterase Activity Studies

Basit Öğe Kaydı
dc.authoridUSLU, HARUN/0000-0001-8827-8557
dc.authoridORHAN, ILKAY ERDOGAN/0000-0002-7379-5436
dc.authoridOzdemir, Zenyep/0000-0003-4559-2305
dc.authoridBozbey Merde, İrem/0000-0002-9290-938X
dc.authoridSenol Deniz, F. Sezer/0000-0002-5850-9841
dc.authoridOzcelik, Azime Berna/0000-0002-3160-5753
dc.authorwosidUSLU, HARUN/P-3681-2019
dc.authorwosidORHAN, ILKAY ERDOGAN/H-6092-2011
dc.authorwosidOzdemir, Zenyep/AAJ-6384-2020
dc.authorwosidBozbey Merde, İrem/HCI-8239-2022
dc.authorwosidSenol Deniz, F. Sezer/AAG-5636-2019
dc.contributor.authorBozbey, Irem
dc.contributor.authorOzdemir, Zeynep
dc.contributor.authorUslu, Harun
dc.contributor.authorOzcelik, Azime Berna
dc.contributor.authorSenol, Fatma Sezer
dc.contributor.authorOrhan, Ilkay Erdogan
dc.contributor.authorUysal, Mchtap
dc.date.accessioned2024-08-04T20:48:44Z
dc.date.available2024-08-04T20:48:44Z
dc.date.issued2020
dc.departmentİnönü Üniversitesien_US
dc.description.abstractBackground: Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are known to be serine hydrolase enzymes responsible for the hydrolysis of acetylcholine (ACh), which is a significant neurotransmitter for regulation of cognition in animals. Inhibition of cholinesterases is an effective method to curb Alzheimer's disease, a progressive and fatal neurological disorder. Objective: In this study, 30 new hydrazone derivatives were synthesized. Then we evaluated their anticholinesterase activity of compounds. We also tried to get insights into binding interactions of the synthesized compounds in the active site of both enzymes by using molecular docking approach. Methods: The compounds were synthesized by the reaction of various substituted/nonsubstituted benzaldehydes with 6-(substitute/nonsubstituephenyl)-3(2H)-pyridazinone-2-yl propiyohydrazide. Anticholinesterase activity of the compounds was determined using Ellman's method. Molecular docking studies were done by using the ADT package version 1.5.6rc3 and showed by Maestro. RMSD values were obtained using Lamarckian Genetic Algorithm and scoring function of AutoDock 4.2 release 4.2.5.1 software. Results: The activities of the compounds were compared with galantamine as cholinesterase enzyme inhibitor, where some of the compounds showed higher BChE inhibitory activity than galantamine. Compound F1(11) was shown to be the best BChE inhibitor effective in 50 mu M dose, providing 89.43% inhibition of BChE (IC50=4.27 +/- 0.36 mu M). Conclusion: This study supports that novel hydrazone derivates may be used for the development of new BChE inhibitory agents.en_US
dc.description.sponsorshipGazi University Scientific Researches Unit [02/2017-22]en_US
dc.description.sponsorshipThis study was funded by Gazi University Scientific Researches Unit. (grant numbers: 02/2017-22).en_US
dc.identifier.doi10.2174/1389557519666191010154444
dc.identifier.endpage1060en_US
dc.identifier.issn1389-5575
dc.identifier.issn1875-5607
dc.identifier.issue11en_US
dc.identifier.pmid31660824en_US
dc.identifier.scopus2-s2.0-85088272463en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.startpage1042en_US
dc.identifier.urihttps://doi.org/10.2174/1389557519666191010154444
dc.identifier.urihttps://hdl.handle.net/11616/99420
dc.identifier.volume20en_US
dc.identifier.wosWOS:000551675400008en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherBentham Science Publ Ltden_US
dc.relation.ispartofMini-Reviews in Medicinal Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectAlzheimer's diseaseen_US
dc.subjectAChE inhibitoren_US
dc.subjectBChE inhibitoren_US
dc.subject3(2H)-Pyridazinoneen_US
dc.subjecthydrazoneen_US
dc.subjectmolecular dockingen_US
dc.titleA Series of New Hydrazone Derivatives: Synthesis, Molecular Docking and Anticholinesterase Activity Studiesen_US
dc.typeArticleen_US

Dosyalar

Koleksiyon

WoS İndeksli Yayınlar Koleksiyonu
PubMed İndeksli Yayın Koleksiyonu
Scopus İndeksli Yayınlar Koleksiyonu