Identification of 1-arylmethyl-3- (2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists |
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| Authors: | Zhu Yun-Fei Gross Timothy D Guo Zhiqiang Connors Patrick J Gao Yinghong Tucci Fabio C Struthers R Scott Reinhart Greg J Saunders John Chen Ta Kung Killam Bonneville Anne L Chen Chen |
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| Affiliation: | Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 10555 Science Center Drive, San Diego, California 92121, USA. fzhu@neurocrine.com |
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| Abstract: | Based on SAR from bicyclic GnRH antagonists such as 6-aminomethyl-7-arylpyrrolo[1,2-a]pyrimid-4-ones (1) and 2-aryl-3-aminomethylimidazolo[1,2-a]pyrimid-5-ones (2a,b), a series of novel uracil compounds (4) were derived as the GnRH antagonists. Their syntheses and initial SAR are discussed herein. This is the first time that monocycle-based GnRH receptor antagonists are reported. |
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