Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production
- 作者：Lain-Yen Hu ; Huangshu John Lei ; Daniel Du ; Theodore R. Johnson ; Victor Fedij ; Catherine Kostlan ; Wen Song Yue ; Mark Lovdahl ; Jie Jack Li ; Mathew Carroll ; Danielle Dettling ; Jeffrey Asbill ; Conglin Fan
- 关键词：Hair growth ; Sebum reduction ; Androgen antagonist ; Amino-pyridine
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 期刊代码：10_0960894x
- 类别：ch
- 出版时间：15 October 2007
- 卷：17
- 期：20
- 页码：5693-5697
- 文件大小：423 K
摘要
A series of amino-pyridines were synthesized and evaluated for androgen antagonist activities. Among these compounds, (R)-(+)-6-[methyl-(1-phenyl-ethyl)-amino]-4-trifluoromethyl-nicotinonitrile was the most active example of this class. This compound displayed potent androgen receptor antagonist activity as well as favorable pharmacokinetic characteristics for a potential topical agent. It also demonstrated remarkable potency for stimulating hair growth in a male C3H mouse model as well as reducing sebum production in the male Syrian hamster ear model.