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. 2008 Jun 1;18(11):3301-5.
doi: 10.1016/j.bmcl.2008.04.036. Epub 2008 Apr 26.

Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity

Chen Chen  1 , Yongsheng Chen, Joseph Pontillo, Zhiqiang Guo, Charles Q Huang, Dongpei Wu, Ajay Madan, Takung Chen, Jenny Wen, Qiu Xie, Fabio C Tucci, Martin Rowbottom, Yun-Fei Zhu, Warren Wade, John Saunders, Haig Bozigian, R Scott Struthers
Affiliations

Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity

Chen Chen et al. Bioorg Med Chem Lett. .

Abstract

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 K(i) of 2.2 nM at GnRH-R and an IC(50) of 36 microM at CYP3A4.

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