Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373483 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Structure–activity relationships for a series of pyrazine carboxamide CB1 antagonists are reported. Pharmaceutical properties of the series are improved via inclusion of hydroxyl-containing sidechains. This structural modification sufficiently improved ADME properties of an orally inactive series such that food intake reduction was achieved in rat feeding models. Compound 35 elicits a 46% reduction in food intake in ad libidum fed rats 4-h post-dose.
Graphical abstractStructure–activity relationships for a series of pyrazine carboxamide CB1 antagonists are reported. Pharmaceutical properties of the series are improved via inclusion of hydroxyl-containing sidechains. This structural modification sufficiently improved ADME properties of an orally inactive series such that food intake reduction was achieved in rat feeding models. Compound 35 elicits a 46 in ad libidum fed rats 4-h post-dose.Figure optionsDownload full-size imageDownload as PowerPoint slide