Clasby Martin C, Chackalamannil Samuel, Czarniecki Michael, Doller Darío, Eagen Keith, Greenlee William J, Lin Yan, Tagat Jayaram R, Tsai Hsingan, Xia Yan, Ahn Ho-Sam, Agans-Fantuzzi Jacqueline, Boykow George, Chintala Madhu, Hsieh Yunsheng, McPhail Andrew T
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Bioorg Med Chem Lett. 2007 Jul 1;17(13):3647-51. doi: 10.1016/j.bmcl.2007.04.061. Epub 2007 Apr 25.
The synthesis and biological activity of a novel series of thrombin receptor antagonists is described. This series of compounds showed excellent in vitro and in vivo potency. The most potent compound 40 had an IC(50) of 7.6 nM and showed robust inhibition of platelet aggregation in a cynomolgus monkey model after oral administration.
描述了一系列新型凝血酶受体拮抗剂的合成及其生物活性。该系列化合物在体外和体内均表现出优异的效力。最有效的化合物40的IC（50）为7.6 nM，在食蟹猴模型中口服给药后对血小板聚集有强烈抑制作用。
