Bahekar Rajesh H, Jain Mukul R, Gupta Arun A, Goel Ashish, Jadav Pradip A, Patel Dipam N, Prajapati Vijay M, Patel Pankaj R
Zydus Research Centre, Cadila Healthcare Ltd., Moraiya, Ahmedabad, India.
Arch Pharm (Weinheim). 2007 Jul;340(7):359-66. doi: 10.1002/ardp.200700024.
Two series of 3,6,7-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 be identical to that of the standard compound (6,7-dichloro-2-trifluromethyl-3-(5-methyl-1,3,4-thiadiazo-2-ylsulfanyl)-quinoxaline (1)).
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都在基于RIN5F细胞的葡萄糖依赖性促胰岛素分泌活性测定中进行了体外筛选。化合物2a-l表现出显著的浓度和葡萄糖依赖性胰岛素分泌效应，并且发现化合物2l的促胰岛素分泌活性与标准化合物(6,7-二氯-2-三氟甲基-3-(5-甲基-1,3,4-噻二唑-2-基硫烷基)喹喔啉(1))相同。
