Author/Authors :
Zhiqiang Guo، نويسنده , , Yun-Fei Zhu، نويسنده , , Fabio C. Tucci، نويسنده , , Yinghong Gao، نويسنده , , R. Scott Struthers، نويسنده , , John Saunders، نويسنده , , Timothy D. Gross، نويسنده , , Qiu Xie، نويسنده , , Greg J. Reinhart، نويسنده , , Chen Chen، نويسنده ,
Abstract :
The novel synthesis and SAR studies of 6-methyluracils as human GnRH receptor antagonists are discussed. Introduction of a small methyl substituent at the β-position from N3 of the uracil improved the GnRH binding potency by 5- to 10-fold. The best compound from the series had binding affinity of 5 nM (Ki) to the human GnRH receptor.
