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Thienopyrimidinone bis-aminopyrrolidine ureas as potent melanin-concentrating hormone receptor-1 (MCH-R1) antagonists |
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| Authors: | Zhang Mingzhu Tamiya Junko Nguyen Linh Rowbottom Martin W Dyck Brian Vickers Troy D Grey Jonathan Schwarz David A Heise Christopher E Haelewyn Jason Mistry Monica S Goodfellow Val S |
| Affiliation: | Department of Medicinal Chemistry, Pharmacology and Molecular Biology, Neurocrine Biosciences Inc., 12790 El Camino Real, San Diego, CA 92130, USA. |
| Abstract: | A series of thienopyrimidinone bis-aminopyrrolidine ureas were designed, synthesized, and evaluated for their ability to bind melanin-concentrating hormone receptor-1. These compounds exhibit potent binding affinity (K(i)=3 nM) and good in vitro metabolic stability. |
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