352303-76-5Relevant academic research and scientific papers
5-Aryluracils as potent GnRH antagonists-Characterization of atropisomers
Zhao, Liren,Guo, Zhiqiang,Chen, Yongsheng,Hu, Tao,Wu, Dongpei,Zhu, Yun-Fei,Rowbottom, Martin,Gross, Timothy D.,Tucci, Fabio C.,Struthers, R. Scott,Xie, Qiu,Chen, Chen
scheme or table, p. 3344 - 3349 (2009/04/11)
Optimization of a series of uracils bearing a 2-fluoro- or 2-chloro-3-methoxyphenyl group at the 5-position resulted in compounds such as 3d and 3f with subnanomolar binding affinity at the human GnRH receptor. While the 2-fluoro-3-methoxyphenyl compound 3a was characterized as a mixture of interchangeable atropisomers, the diastereoisomers of 2-chloro-3-methoxyphenyl analogs were separated. It was found that the aR-atropisomer was much more potent than the aS-isomer based on the X-ray crystal structure of 3h-II.
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
