Author/Authors :
Ruo Xu، نويسنده , , Shengjian Li، نويسنده , , Jaroslava Paruchova، نويسنده , , Mark D. McBriar، نويسنده , , Henry Guzik، نويسنده , , Anandan Palani، نويسنده , , John W. Clader، نويسنده , , Kathleen Cox، نويسنده , , William J. Greenlee، نويسنده , , Brian E. Hawes، نويسنده , , Timothy J. Kowalski، نويسنده , , Kim O’Neill، نويسنده , , Brian D. Spar، نويسنده , , Blair Weig، نويسنده , , Daniel J. Weston، نويسنده ,
Abstract :
Melanin concentrating hormone (MCH) receptor antagonists have been proposed as potential treatments of obesity. MCH receptor antagonists with a biphenylamine subunit have been reported previously at Schering-Plough. Herein, we report the discovery of bicyclo[4.1.0]heptanes as replacements for the middle phenyl ring of the biphenylamine moiety in order to eliminate its potential mutagenic liability. Structure–activity relationships in this series were found to be very similar to those of the original biphenylamine series, suggesting that the two series have similar binding modes.
