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Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers |
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| Authors: | 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 |
| Affiliation: | Department of Medicinal Chemistry, Neurocrine Biosciences, Inc. 12790 El Camino Real, San Diego, CA 92130, USA. |
| Abstract: | 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). |
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