855230-52-3Relevant academic research and scientific papers
Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties
Regan, Colin F.,Guo, Zhiqiang,Chen, Yongsheng,Huang, Charles Q.,Chen, Mi,Jiang, Wanlong,Rueter, Jaimie K.,Coon, Timothy,Chen, Chen,Saunders, John,Brown, Michael S.,Betz, Steve F.,Struthers, R. Scott,Yang, Chun,Wen, Jenny,Madan, Ajay,Zhu, Yun-Fei
scheme or table, p. 4503 - 4507 (2009/04/06)
A novel series of potent zwitterionic uracil GnRH antagonists were discovered that showed reduced liability for CYP3A4 enzyme inhibition.
Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers
Guo, Zhiqiang,Chen, Yongsheng,Huang, Charles Q.,Gross, Timothy D.,Pontillo, Joseph,Rowbottom, Martin W.,Saunders, John,Struthers, Scott,Tucci, Fabio C.,Xie, Qiu,Wade, Warren,Zhu, Yun-Fei,Wu, Dongpei,Chen, Chen
, p. 2519 - 2522 (2007/10/03)
Uracil derivatives were designed and synthesized to avoid atropisomers observed in the 6-methyluracils as antagonists of the human GnRH receptor. Optimization at the 1- and 5-positions of the uracil resulted in potent compounds such as 24 (Ki = 0.45 nM).
