Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119

…, B Fioravanti, G Pereira, I Calderon, J Uy…

文献索引：Semple, Graeme; Fioravanti, Beatriz; Pereira, Guillherme; Calderon, Imelda; Uy, Jane; Choi, Karoline; Xiong, Yifeng; Ren, Albert; Morgan, Michael; Dave, Vibha; Thomsen, William; Unett, David J.; Xing, Charles; Bossie, Stuart; Carroll, Chris; Chu, Zhi-Liang; Grottick, Andrew J.; Hauser, Erin K.; Leonard, James; Jones, Robert M. Journal of Medicinal Chemistry, 2008 , vol. 51, # 17 p. 5172 - 5175

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被引用次数: 106

摘要

GPR119 is a rhodopsin-like GPCR expressed in pancreatic β-cells and incretin releasing cells in the GI tract. As with incretins, GPR119 increases cAMP levels in these cell types, thus making it a highly attractive potential target for the treatment of diabetes. The discovery of the first reported potent agonist of GPR119, 2-fluoro-4-methanesulfonyl-phenyl)-{6-[4-(3- isopropyl-[1, 2, 4] oxadiazol-5-yl)-piperidin-1-yl]-5-nitro-pyrimidin-4-yl}-amine (8g, ...