1041863-07-3Relevant academic research and scientific papers
Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity
Chen, Chen,Chen, Yongsheng,Pontillo, Joseph,Guo, Zhiqiang,Huang, Charles Q.,Wu, Dongpei,Madan, Ajay,Chen, Takung,Wen, Jenny,Xie, Qiu,Tucci, Fabio C.,Rowbottom, Martin,Zhu, Yun-Fei,Wade, Warren,Saunders, John,Bozigian, Haig,Struthers, R. Scott
body text, p. 3301 - 3305 (2009/04/06)
Incorporation of a carboxylic acid into a series of uracil derivatives as hGnRH-R antagonists resulted in a significant reduction of CYP3A4 inhibitory activity. Highly potent hGnRH antagonists with low CYP3A4 inhibitory liability, such as 8a and 8d, were identified. Thus, 8a had a Ki of 2.2 nM at GnRH-R and an IC50 of 36 μM at CYP3A4.
