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Bis(aminopyrrolidine)-derived ureas (APUs) as potent MCH1 receptor antagonists |
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| Authors: | Grey Jonathan Dyck Brian Rowbottom Martin W Tamiya Junko Vickers Troy D Zhang Mingzhu Zhao Liren Heise Christopher E Schwarz David Saunders John Goodfellow Val S |
| Affiliation: | Department of Medicinal Chemistry, Neurocrine Biosciences Inc., 12790 El Camino Real, San Diego, CA 92130, USA. |
| 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). |
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