Discovery of Sodium R-(+)-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl] benzyl)-4-methyl-2, 6-dioxo-3, 6-dihydro-2 H-pyrimidin-1-yl]-1- …

C Chen, D Wu, Z Guo, Q Xie, GJ Reinhart…

Index: Chen, Chen; Wu, Dongpei; Guo, Zhiqiang; Xie, Qiu; Reinhart, Greg J.; Madan, Ajay; Wen, Jenny; Chen, Takung; Huang, Charles Q.; Chen, Mi; Chen, Yongsheng; Tucci, Fabio C.; Rowbottom, Martin; Pontillo, Joseph; Zhu, Yun-Fei; Wade, Warren; Saunders, John; Bozigian, Haig; Struthers, R. Scott Journal of Medicinal Chemistry, 2008 , vol. 51, # 23 p. 7478 - 7485

Full Text: HTML

Citation Number: 43

Abstract

The discovery of novel uracil phenylethylamines bearing a butyric acid as potent human gonadotropin-releasing hormone receptor (h GnRH-R) antagonists is described. A major focus of this optimization was to improve the CYP3A4 inhibition liability of these uracils while maintaining their GnRH-R potency. R-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6- [trifluoromethyl] benzyl)-4-methyl-2, 6-dioxo-3, 6-dihydro-2 H-pyrimidin-1-yl]-1- ...