期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 6, 页码 1784-1787出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.12.045
关键词
SARM; benzimidazoles; in vivo screening
The synthesis and in vivo SAR of 2-(2,2,2)-trifluoroethyl-benzimidazoles are described. Prostate antagonism and/or levator am agonism can be modulated by varying the substitution at the 2-position of 5,6-dichloro-benzimidazoles. Potent androgen agonists on the muscle were discovered that strongly bind to the androgen receptor (2-17 nM) and show potent in vivo efficacy (0.03-0.11 mg/day). True SARMs showing both prostate antagonism and levator am agonism were revealed. (c) 2006 Elsevier Ltd. All rights reserved.
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