| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1362545 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
A new series of 5-(pyridinon-1-yl)indazoles with MCH-1 antagonist activity were synthesized. Potential cardiovascular risk for these compounds was assessed based upon their interaction with the hERG potassium channel in a mini-patch clamp assay. Selected compounds were studied in a 5-day diet-induced obese mouse model to evaluate their potential use as weight loss agents. Structural modification of the 5-(pyridinon-1-yl)indazoles to give 5-(furopyridinon-5-yl)indazoles provided compounds with enhanced pharmacokinetic properties and improved efficacy.
Graphical abstractThe synthesis and SAR of 5-(pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as potent MCH-1 antagonists are described.Figure optionsDownload full-size imageDownload as PowerPoint slide
