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ID: ALA1141988

Journal: Bioorg Med Chem Lett

Title: Bis(aminopyrrolidine)-derived ureas (APUs) as potent MCH1 receptor antagonists.

Authors: Grey J, Dyck B, Rowbottom MW, Tamiya J, Vickers TD, Zhang M, Zhao L, Heise CE, Schwarz D, Saunders J, Goodfellow VS.

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 MCH(1) receptor. The series was optimized for substitution and stereochemistry to generate a functional antagonist with a K(i) of 3.3 nM and IC(50) of 12 nM (GTPgammaS).

CiteXplore: 15686900

DOI: 10.1016/j.bmcl.2004.12.036