环加成
苯二氮卓
对接(动物)
化学
组合化学
表征(材料科学)
1,3-偶极环加成
立体化学
计算化学
材料科学
纳米技术
催化作用
有机化学
生物化学
医学
受体
护理部
作者
Marouane Ait Lahcen,Mohamed Adardour,Salma Mortada,Mehdi Oubahmane,Samir Hmaimou,Mohamed Loughzail,Ismail Hdoufane,Sanae Lahmidi,My El Abbes Faouzi,Driss Cherqaoui,Joel T. Mague,A. Baouid
标识
DOI:10.1080/07391102.2023.2203263
摘要
We report in this work a synthesis of novel triazolo[1,5]benzodiazepine derivatives by the 1,3-dipolar cycloaddition reaction of N-aryl-C-ethoxycarbonylnitrilimines with 1,5-benzodiazepines. All the structures of the new compounds were determined from their NMR (1H and 13C) and HRMS. Then, X-ray crystallography analysis of compound 4d confirmed the stereochemistry of cycloadducts. The compounds 1, 4a–d, 5a–d, 6c, 7 and 8 were evaluated for their in vitro anti-diabetic activity against α-glucosidase. The compounds 1, 4d, 5a and 5b showed potential inhibitory activities compared to standard acarbose. Additionally, an in silico docking study was conducted to look into the active binding mode of the synthesized compounds within the target enzyme.
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