Identification of 1-arylmethyl-3- (2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists.
Identification of 1-arylmethyl-3- (2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists.
复制标题
鉴定 1-芳基甲基-3-(2-氨基乙基)-5-芳基尿嘧啶作为新型促性腺激素释放激素受体拮抗剂。
DOI:
10.1021/jm034041s
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发表时间:
2003
期刊:
影响因子:
--
通讯作者:
Chen,Chen
中科院分区:
文献类型:
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作者:
Zhu,Yun-Fei;Gross,TimothyD;Guo,Zhiqiang;ConnorsJr,PatrickJ;Gao,Yinghong;Tucci,FabioC;Struthers,RScott;Reinhart,GregJ;Saunders,John;Chen,TaKung;KillamBonneville,AnneL;Chen,Chen
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.