Synthesis and Antidiabetic Activity of 3,6,7-Trisubstituted-2-(1H-imidazol-2-ylsulfanyl)quinoxalines and Quinoxalin-2-yl isothioureas
作者:Rajesh H. Bahekar、Mukul R. Jain、Arun A. Gupta、Ashish Goel、Pradip A. Jadav、Dipam N. Patel、Vijay M. Prajapati、Pankaj R. Patel
DOI:10.1002/ardp.200700024
日期:2007.7
7‐trisubstituted‐2‐(1H‐imidazol‐2‐ylsulfanyl)‐quinoxalines 2a‐l and 2‐(quinoxalin‐2‐yl)‐isothioureas 3a‐l were prepared. All the test compounds 2a‐l and 3a‐l were screened in vitro, in a RIN5F cell‐based assay for glucose‐dependent insulinotropic activity. A significant concentration and glucose‐dependent insulin secretion effect was seen with compounds 2a‐l and the insulinotropic activity of compound 2l was found to
制备了两个系列的 3,6,7-三取代-2-(1H-咪唑-2-基硫烷基)-喹喔啉2a-l 和2-(喹喔啉-2-基)-异硫脲3a-l。所有测试化合物 2a-l 和 3a-l 都在体外筛选,在基于 RIN5F 细胞的测定中进行葡萄糖依赖性促胰岛素活性。化合物 2a-l 具有显着的浓度和葡萄糖依赖性胰岛素分泌作用,并且发现化合物 2l 的促胰岛素活性与标准化合物(6,7-二氯-2-三氟甲基-3-(5 -Methyl-1,3,4-thiadiazo-2-ylsulfanyl) -quinoxaline (1))。