| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372832 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
A series of 1,3-disubstituted-1H-pyrrole-based antagonists of the human Melanin-Concentrating Hormone Receptor 1 (h-MCH-R1) are reported. High-throughput screening of the AstraZeneca compound collection yielded 1, a hit with moderate affinity towards MCH-R1. Subsequent structural manipulations and SAR analysis served to rationalize potency requirements, and 12 was identified as a novel, functional MCH-R1 antagonist with favorable pharmacokinetic properties.
Graphical abstractThe optimization of an HTS-derived hit compound into a potent and metabolically stable MCH-R1 antagonist is described.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Organic Chemistry
Authors
Susanne Berglund, Bryan J. Egner, Henrik Gradén, Joakim Gradén, David G.A. Morgan, Tord Inghardt, Fabrizio Giordanetto,