Author/Authors :
Yun-Fei Zhu، نويسنده , , R. Scott Struthers، نويسنده , , Patrick J. Connors Jr.، نويسنده , , Yinghong Gao، نويسنده , , Timothy D. Gross، نويسنده , , John Saunders، نويسنده , , Keith Wilcoxen، نويسنده , , Greg J. Reinhart، نويسنده , , Nicholas Ling، نويسنده , , Chen Chen، نويسنده ,
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 (Ki) binding affinity to human GnRH receptor.