Design, synthesis, characterization, biological evaluation, and molecular docking studies of novel 1,2-aminopropanthiols substituted derivatives as selective carbonic anhydrase, acetylcholinesterase and α-glycosidase enzymes inhibitors
作者:Afat Huseynova、Ruya Kaya、Parham Taslimi、Vagif Farzaliyev、Xadija Mammadyarova、Afsun Sujayev、Burak Tüzün、Umit M. Kocyigit、Saleh Alwasel、İlhami Gulçin
DOI:10.1080/07391102.2020.1811772
日期:2022.1.2
an anti-Alzheimer’s disease substance were also recorded revealing strong carbonic anhydrase I, and II, α-glycosidase, and acetylcholinesterase inhibitory effects. These synthesized novel 1,2-aminopropanthiols substituted derivatives (1a–g) were found to be effective inhibitors for the α-glycosidase, human carbonic anhydrase I and II, and acetylcholinesterase enzymes, with Ki values in the range of
摘要 在本文中,1,2-氨基丙硫醇 ( 1a-g ) 的各种取代衍生物已通过一种通用且有效的方法一步制备,从可用的硫杂环丙烷和芳族胺(苯胺、邻甲苯胺)作为一种方便的硫和氮的来源。合成的化合物通过光谱和分析数据进行了充分表征。合成了七种新化合物。还记录了表明它们构成抗阿尔茨海默病物质的潜力的生化特性,显示出强的碳酸酐酶 I 和 II、α-糖苷酶和乙酰胆碱酯酶抑制作用。这些合成的新型 1,2-氨基丙硫醇取代衍生物 ( 1a-g) 被发现是 α-糖苷酶、人碳酸酐酶 I 和 II 以及乙酰胆碱酯酶的有效抑制剂,α-糖苷酶的 K i值范围为 11.47 ± 0.87–24.09 ± 6.37 µM,29.30 ± 4.67-79.01 hCA I 为 ± 4.49 µM,hCA II 为 14.27 ± 2.82-30.85 ± 12.24 µM,AChE 为 5.76 ± 1.55–55.39 ±