… derived human GnRH receptor antagonists:(R)-3-[2-(2-amino) phenethyl]-1-(2, 6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5

…, M Moorjani, O Acevedo, L Carter, SK Sullivan…

Index: Rowbottom, Martin W.; Tucci, Fabio C.; Connors Jr., Patrick J.; Gross, Timothy D.; Zhu, Yun-Fei; Guo, Zhiqiang; Moorjani, Manisha; Acevedo, Oscar; Carter, Lee; Sullivan, Susan K.; Xie, Qiu; Fisher, Andrew; Struthers, R. Scott; Saunders, John; Chen, Chen Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 19 p. 4967 - 4973

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Citation Number: 12

Abstract

The synthesis of a series of (R)-3-[2-(2-amino) phenethyl]-1-(2, 6-difluorobenzyl)-6- methyluracils containing a substituted thiophene or thiazole at C-5 is described. SAR around C-5 of the uracil led to the discovery that a 2-thienyl or (2-phenyl) thiazol-4-yl group is required for optimal receptor binding. The best compound from the series had a binding affinity of 2nM (Ki) for the human GnRH receptor. A novel and convenient preparation of N ...