1556953-99-1Relevant academic research and scientific papers
Improving the pharmacokinetics of GPR40/FFA1 full agonists
Du, Xiaohui,Dransfield, Paul J.,Lin, Daniel C.-H.,Wong, Simon,Wang, Yingcai,Wang, Zhongyu,Kohn, Todd,Yu, Ming,Brown, Sean P.,Vimolratana, Marc,Zhu, Liusheng,Li, An-Rong,Su, Yongli,Jiao, Xianyun,Liu, Jiwen,Swaminath, Gayathri,Tran, Thanhvien,Luo, Jian,Zhuang, Run,Zhang, Jane,Guo, Qi,Li, Frank,Connors, Richard,Medina, Julio C.,Houze, Jonathan B.
, p. 384 - 389 (2014/05/06)
We recently reported the discovery of a potent GPR40 full agonist AM-1638 (1). Herein, we describe our efforts in improving the drug-like properties of the full agonists through the systematic introduction of polar groups in the C-, D-, and A-rings. This led to the discovery of new GPR40 full agonists with significantly improved pharmacokinetic propeties. Compound 8 and 20 also showed potent in vivo efficacy in oral glucose tolerance tests in mice in addition to the improvement in properties.
