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Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzymeBozbey, İremÖnel, Gülce TaşkorTürkmenoğlu, BurçinGürsoy, ŞuleDilek, EsraErgün, MuhammedÖzçelik, Azime BernaUysal, MehtapAcetylcholinesterasealzheimer’s diseasemolecular dockingpyridazinonetriazole2 [[4 (3 bromophenyl) 5 thioxo 4,5 dihydro 1h 1,2,4 triazol 3 yl]methyl] 6 [4 (4 chlorophenyl)piperazin 1 yl]pyridazin 3(2h) one2 [[4 (4 bromophenyl) 5 thioxo 4,5 dihydro 1h 1,2,4 triazol 3 yl]methyl] 6 [4 (4 chlorophenyl)piperazin 1 yl]pyridazin 3(2h) one3(2h)pyridazinone triazole6 [4 (4 chlorophenyl)piperazin 1 yl] 2 [(4 phenyl 6 thioxo 4,5 dihydro 1h 1,2,4 triazol 3 yl)methyl]pyridazin] 3(2h) one6 [4 (4 chlorophenyl)piperazin 1 yl] 2 [[4 (2 methoxyphenyl)-5-thioxo-4,5-dihydro 1h 1,2,4 triazol 3 yl]methyl]pyridazin 3(2h) one6 [4 (4 chlorophenyl)piperazin 1 yl] 2 [[4 (3 methoxyphenyl)-5-thioxo-4,5-dihydro 1h 1,2,4 triazol 3 yl]methyl]pyridazin 3(2h) one6 [4 (4 chlorophenyl)piperazin 1 yl] 2 [[5 thioxo 4 [4 (trifluoromethoxy)phenyl] 4,5 dihydro 1h 1,2,4 triazol 3 yl]methyl]pyridazin 3(2h) onecholinesterase inhibitortacrinetriazole derivativeunclassified drugArticlecarbon nuclear magnetic resonancecrystal structureenzyme inhibitionIC50inhibition constantmass spectrometryproton nuclear magnetic resonanceAlzheimer'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 by1H-NMR,13C-NMR, 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 µM. The compound with the best inhibitory properties was compound 6d with a Ki value of 2.35 ± 0.18 µM. 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). © 2022 Marmara University Press.Marmara University2022Articlehttps://rdlopen.rawdatalibrary.net/r/ebyu/12627https://doi.org/10.29228/jrp.2392630-6344enJournal of Research in Pharmacyinfo:eu-repo/semantics/openAccessinfo:eu-repo/semantics/articlehttps://ebyu-rdlopen.rawdatalibrary.net/tr/items/ebyu/12627