Title of article :
Design, synthesis and structure–Activity relationships of novel imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists
Author/Authors :
Timothy D. Gross، نويسنده , , Yun-Fei Zhu، نويسنده , , John Saunders، نويسنده , , Keith M. Wilcoxen، نويسنده , , Yinghong Gao، نويسنده , , Patrick J. Connors Jr.، نويسنده , , Zhiqiang Guo، نويسنده , , R. Scott Struthers، نويسنده , , Greg J. Reinhart، نويسنده , , Chen Chen، نويسنده ,
Abstract :
SAR studies of lead GnRH receptor antagonists 2a and 2b reported earlier resulted in the discovery of compound 10b which showed much higher potency (Ki=4.6 nM, compared with 2b, Ki=230 nM) in which the 7-position of the imidazolo[1,2-a]pyrimidone core was substituted with a methyl group, and the ester at the 6-position was replaced by the 3-methoxyphenyl group.
