an anti-Alzheimer’s disease substance were also recorded revealing strong carbonicanhydrase 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 carbonicanhydrase 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 ±
Direct annulation between glycine derivatives and thiiranes through photoredox/iron cooperative catalysis
A visible-light-induced aerobic oxidative [2+3] cycloaddition reaction between glycine derivatives and thiiranes has been disclosed, which provides an efficient and atom-economical strategy for the rapid synthesis of thiazolidine-2-carboxylic acid derivatives and the post-modification of glycine-derived dipeptides under mild conditions with good yield and high diastereoselectivities. A preliminary