Bioorganic & Medicinal Chemistry Letters 2002-02-11

Initial structure-activity relationship studies of a novel series of pyrrolo[1,2-a]pyrimid-7-ones as GnRH receptor antagonists.

Yun-Fei Zhu, R Scott Struthers, Patrick J Connors, Yinghong Gao, Timothy D Gross, John Saunders, Keith Wilcoxen, Greg J Reinhart, Nicholas Ling, Chen Chen

Index: Bioorg. Med. Chem. Lett. 12(3) , 399-402, (2002)

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Abstract

Initial SAR studies on 1-aminomethyl-2-aryl-3-cyano-pyrrolo[1,2-a]pyrimid-7-one-6-carboxylates as human GnRH receptor antagonists were discussed. 2-(2-Methylaminoethyl)pyridine was discovered to be a key feature for generating active compounds. The best compound from the series had 25 nM (K(i)) binding affinity to human GnRH receptor.