单胺氧化酶
乙酰胆碱酯酶
印丹
化学
单胺氧化酶B
酶
阿切
药理学
噻唑
立体化学
生物化学
医学
作者
İsmail Okan Ateş,Asaf Evrim Evren,Begüm Nurpelin Sağlık,Leyla Yurttaş
标识
DOI:10.1515/znc-2021-0058
摘要
Abstract Although radical treatment of Alzheimer’s and Parkinson’s disease is not possible yet, it is aimed to slow the course of the disease and increase the life quality of individuals with the drugs used in the clinic at the present time. Successful results have been achieved in the use of cholinesterase inhibitors and monoamine oxidase inhibitors together in these neurodegenerative diseases. In this study, indane ring which are in the structure of anticholinesterase effective molecules and 2-hydrazinothiazole structure whose inhibitory activities reported on monoamine oxidase-B (MAO-B) were combined; 4-(substituted phenyl)-2-[2-(3-phenyl-2,3-dihydro-1H-inden-1-ylidene) hydrazinyl]thiazole derivatives (3a–3i) were synthesized as dual inhibitors. The structures of the compounds were verified by IR, 1H-NMR, 13C-NMR, and HRMS spectroscopy. When enzyme inhibition activities were evaluated, it was determined that the compounds 3a (42.33%) and 3d (42.39%) on acetylcholinesterase (AChE) enzyme; compounds 3g (75.42%) and 3h (60.33%) showed inhibition on MAO-B enzyme at most, at 10−3 M concentration.
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