College of Pharmacy, Kangwon National University, Chunchon 200-701, Republic of Korea.
Bioorg Med Chem. 2013 Mar 1;21(5):1349-56. doi: 10.1016/j.bmc.2012.12.013. Epub 2012 Dec 20.
GPR119 agonist has emerged as a promising target for the treatment of type 2 diabetes. A series of novel 2,4-disubstituted quinazoline analogues was prepared and evaluated their agonistic activity against human GPR119. The analogues bearing azabicyclic amine substituents (12a, 12c and 12g) exhibited better EC(50) values than that of OEA though they appeared to be partial agonists.
GPR119 激动剂已成为治疗 2 型糖尿病的有希望的靶点。一系列新型 2,4-二取代喹唑啉类似物被制备并评估了它们对人 GPR119 的激动活性。尽管含有氮杂双环胺取代基的类似物（12a、12c 和 12g）似乎为部分激动剂，但它们表现出比 OEA 更好的 EC(50) 值。
