Synthesis and Structure–activity relationships of 1-arylmethyl-3-(1-methyl-2-amino) ethyl-5-aryl-6-methyluracils as antagonists of the human GnRH Receptor

…, RS Struthers, GJ Reinhart, J Saunders, C Chen

Index: Tucci, Fabio C.; Zhu, Yun-Fei; Guo, Zhiqiang; Gross, Timothy D.; Connors Jr., Patrick J.; Struthers, R. Scott; Reinhart, Greg J.; Saunders, John; Chen, Chen Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 19 p. 3317 - 3322

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Citation Number: 27

Abstract

A new class of small molecule GnRH antagonists, the 1-arylmethyl-3-(1-methyl-2-amino) ethyl-5-aryl-6-methyluracils, was designed and a novel stereoselective synthesis for these compounds was developed. The stereochemical integrities of key intermediates (S)-6 and (R)-6 were confirmed by a combination of X-ray crystallography and chiral HPLC determinations. SAR studies were performed, which allowed the identification of ...

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