期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 20, 页码 5693-5697出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.07.059
关键词
hair growth; sebum reduction; androgen antagonist; amino-pyridine
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. (c) 2007 Elsevier Ltd. All rights reserved.
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