Author/Authors :
Lain-Yen Hu، نويسنده , , Huangshu John Lei، نويسنده , , Daniel du Plessis، نويسنده , , Theodore R. Johnson، نويسنده , , Victor Fedij، نويسنده , , Catherine Kostlan، نويسنده , , Wen-Song Yue، نويسنده , , Mark Lovdahl، نويسنده , , Jie Jack Li، نويسنده , , Mathew Carroll، نويسنده , , Danielle Dettling، نويسنده , , Jeffrey Asbill، نويسنده , , Conglin Fan، نويسنده , , Kimberly Wade، نويسنده , , David Pocalyko، نويسنده , , Kimberly Lapham، نويسنده , , Radhika Yalamanchili، نويسنده , , Brian Samas، نويسنده , , Derek Vrieze، نويسنده , , Susan Ciotti، نويسنده , , et al.، نويسنده ,
Abstract :
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.
Keywords :
Hair growth , Sebum reduction , Amino-pyridine , Androgen antagonist
