Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1378783 | Bioorganic & Medicinal Chemistry Letters | 2005 | 7 Pages |
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
Authors
Martin W. Rowbottom, Troy D. Vickers, Brian Dyck, Junko Tamiya, Mingzhu Zhang, Liren Zhao, Jonathan Grey, David Provencal, David Schwarz, Christopher E. Heise, Monica Mistry, Andrew Fisher, Teresa Dong, Tao Hu, John Saunders, Val S. Goodfellow,