Article ID Journal Published Year Pages File Type
1378783 Bioorganic & Medicinal Chemistry Letters 2005 7 Pages PDF
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.

Graphical abstractThe design and synthesis of a number of bis-aminopyrrolidine ureas is described and the results from SAR studies are summarized. The best compounds showed Ki = 1 nM.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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