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.
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.
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DOI：
10.1016/s0960-894x(03)00619-x
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发表时间：
2003-10
影响因子：
2.7
通讯作者：
F. Tucci;Yun-fei Zhu;Zhiqian Guo;T. Gross;Patrick J. Connors;R. Struthers;Greg J. Reinhart;J. Saunders-J.
中科院分区：
文献类型：
--
作者：
F. Tucci;Yun-fei Zhu;Zhiqian Guo;T. Gross;Patrick J. Connors;R. Struthers;Greg J. Reinhart;J. Saunders-J.
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 derivatives (R)-9f, (R)-9h and (R)-12 as potent hGnRH antagonists (Ki=20 nM).
