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ID: ALA1140258
Journal: Bioorg Med Chem Lett
Title: Synthesis and structure-activity relationships of biarylcarboxamide bis-aminopyrrolidine urea derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1).
Authors: Rowbottom MW, Vickers TD, Dyck B, Tamiya J, Zhang M, Zhao L, Grey J, Provencal D, Schwarz D, Heise CE, Mistry M, Fisher A, Dong T, Hu T, Saunders J, Goodfellow VS.
Abstract: A novel series of bis-aminopyrrolidine ureas containing either a 4-biphenylcarboxmide or 5-phenyl-2-thiophenecarboxamide group have been identified as potent and functional antagonists of the melanin-concentrating hormone receptor-1. Syntheses and SAR are described, which led to the discovery of compounds with high binding affinity (Ki = 1 nM) for the receptor. Preliminary in vitro metabolic stability data are also reported for key compounds.
CiteXplore: 15950467