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Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 1 |
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| Authors: | Rowbottom Martin W Vickers Troy D Dyck Brian Grey Jonathan Tamiya Junko Zhang Mingzhu Kiankarimi Mehrak Wu Dongpei Dwight Wesley Wade Warren S Schwarz David Heise Christopher E Madan Ajay Fisher Andrew Petroski Robert Goodfellow Val S |
| Institution: | Department of Medicinal Chemistry, Neurocrine Biosciences Inc., San Diego, CA 92130, USA. mrowbottom@neurocrine.com |
| Abstract: | The design, synthesis, and SAR of a series of retro bis-aminopyrrolidine ureas are described. Compounds from this series exhibited potent binding affinity and functional activity at MCH-R1, and good oral bioavailability in rat. |
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| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |