Zhiqian Guo, Yongsheng Chen, Dongpei Wu
Oct 20, 2003
Citations
0
Influential Citations
25
Citations
Quality indicators
Journal
Bioorganic & medicinal chemistry letters
Abstract
The synthesis and SAR studies of thieno[2,3-d]pyrimidine-2,4-diones as human GnRH receptor antagonists to treat reproductive diseases are discussed. It was found that the 2-(2-pyridyl)ethyl group on the 5-aminomethyl functionality of the core structure was a key feature for good receptor binding activity. SAR study of the 6-(4-aminophenyl) group suggests that hydrophobic substituents were preferred. The best compound from this series had binding affinity (K(i)) of 0.4 nM to the human GnRH receptor.