3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization.

@article{Tucci200532RAmino2phenylethyl126difluorobenzy,
  title={3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization.},
  author={F. Tucci and Yun-fei Zhu and R. Struthers and Zhiqian Guo and T. Gross and Martin W Rowbottom and O. Acevedo and Yinghong Gao and J. Saunders and Q. Xie and Greg J. Reinhart and Xin-jun Liu and N. Ling and A. Bonneville and Takung Chen and H. Bozigian and C. Chen},
  journal={Journal of medicinal chemistry},
  year={2005},
  volume={48 4},
  pages={
          1169-78
        }
}
Further structure-activity relationship studies of a series of substituted uracils at the 1, 3, and 5 positions resulted in the discovery of several potent antagonists of the human gonadotropin-releasing hormone receptor. Uracils bearing a side chain derived from phenylglycinol at the 3-position were shown to be orally bioavailable in monkeys. 3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidin-2,4-dione (R-13b, NBI 42902) displayed subnanomolar… Expand
5-Aryluracils as potent GnRH antagonists-Characterization of atropisomers.
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