| Autor: |
Martinborough E; Discovery Research, Ligand Pharmaceuticals Inc., 10275 Science Center Drive, San Diego, California 92121, USA., Shen Y, Oeveren Av, Long YO, Lau TL, Marschke KB, Chang WY, López FJ, Vajda EG, Rix PJ, Viveros OH, Negro-Vilar A, Zhi L |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2007 Oct 18; Vol. 50 (21), pp. 5049-52. Date of Electronic Publication: 2007 Sep 21. |
| DOI: |
10.1021/jm070231h |
| Abstrakt: |
The androgen receptor is a ligand inducible transcription factor that is involved in a broad range of physiological functions. Here we describe the discovery of a new class of orally available selective androgen receptor modulators. The lead compound, 6-[(2R,5R)-2-methyl-5-((R)-2,2,2-trifluoro-1-hydroxyethyl)pyrrolidin-1-yl]-4-trifluoromethylquinolin-2(1H)-one (6a), showed excellent anabolic activity in muscle with reduced effect on the prostate in a rat model of hypogonadism. The compound also improved bone strength in a rat model of post-menopausal osteoporosis. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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