618914-13-9Relevant academic research and scientific papers
Synthesis and structure-activity relationships of uracil 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
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
, p. 4967 - 4973 (2004)
The design and synthesis of a number of 5-thiazolyl and 5-thienyl substituted uracils is described and results from SAR studies are summarized. The best compound showed Ki = 2 nM. The synthesis of a series of (R)-3-[2-(2-amino)phenethyl]-1-(2,6
Synthesis and Structure-Activity Relationships of 1-Arylmethyl-5-aryl-6-methyluracils as Potent Gonadotropin-Releasing Hormone Receptor Antagonists
Guo, Zhiqiang,Zhu, Yun-Fei,Gross, Timothy D.,Tucci, Fabio C.,Gao, Yinghong,Moorjani, Manisha,Connors Jr., Patrick J.,Rowbottom, Martin W.,Chen, Yongsheng,Struthers, R. Scott,Xie, Qiu,Saunders, John,Reinhart, Greg,Chen, Ta Kung,Bonneville, Anne L. Killam,Chen, Chen
, p. 1259 - 1271 (2007/10/03)
Based on the SAR from bicyclic gonadotropin-releasing hormone (GnRH) antagonists such as 6-aminomethyl-7-aryl-pyrrolo [1,2-a] pyrimid-4-ones (5) and 2-aryl-3-aminomethyl-imidazolo-[1,2-a]pyrimid-5-ones (6a,b), a series of novel uracil compounds (8) were d
Synthesis and structure-activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists
Guo, Zhiqiang,Zhu, Yun-Fei,Tucci, Fabio C.,Gao, Yinghong,Struthers, R. Scott,Saunders, John,Gross, Timothy D.,Xie, Qiu,Reinhart, Greg J.,Chen, Chen
, p. 3311 - 3315 (2007/10/03)
The novel synthesis and SAR studies of 6-methyluracils as human GnRH receptor antagonists are discussed. Introduction of a small methyl substituent at the β-position from N3 of the uracil improved the GnRH binding potency by 5- to 10-fold. The best compou
