Author/Authors :
Jonathan Grey، نويسنده , , Brian Dyck، نويسنده , , Martin W. Rowbottom، نويسنده , , Junko Tamiya، نويسنده , , Troy D. Vickers، نويسنده , , Mingzhu Zhang، نويسنده , , Liren Zhao، نويسنده , , Christopher E. Heise، نويسنده , , David Schwarz، نويسنده , , John Saunders، نويسنده , , Val S. Goodfellow، نويسنده ,
Abstract :
Ureas derived from two substituted 3-aminopyrrolidine subunits were prepared as constrained analogs of a linear lead compound and tested as antagonists of the MCH1 receptor. The series was optimized for substitution and stereochemistry to generate a functional antagonist with a Ki of 3.3 nM and IC50 of 12 nM (GTPγS).
Keywords :
obesity , Anxiety , Melanin-concentrating hormone , depression
