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

Martin W. Rowbottom,Troy D. Vickers,Brian Dyck,Jonathan Grey,Junko Tamiya,Mingzhu Zhang,Mehrak Kiankarimi,Dongpei Wu,Wesley Dwight,Warren S. Wade,David Schwarz,Christopher E. Heise,Ajay Madan,Andrew Fisher,Robert Petroski,Val S. Goodfellow

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

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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关键词

Melanin-concentrating hormone (MCH),Melanin-concentrating hormone receptor (MCH-R1),Melanin-concentrating hormone receptor antagonists (MCH-R1 antagonists),Obesity,Aminopyrrolidine urea,Retro aminopyrrolidine urea

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