485404-41-9Relevant articles and documents
Design, synthesis and structure-activity relationships of novel imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists
Gross, Timothy D.,Zhu, Yun-Fei,Saunders, John,Wilcoxen, Keith M.,Gao, Yinghong,Connors Jr., Patrick J.,Guo, Zhiqiang,Struthers,Reinhart, Greg J.,Chen, Chen
, p. 2185 - 2187 (2007/10/03)
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.