| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375334 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
A novel class of cannabinoid-1 (CB1) receptor antagonists for the treatment of obesity is presented. The carboxamide linker in a set of 5,6-diaryl-pyrazine-2-amide derivatives was transformed into the corresponding thioamide, by using a one-pot synthesis. The structural series of thioamides not only showed retained CB1 potency (below 10 nM), but also showed improved solubility. In addition, the neutral antagonist 2c significantly reduced body weight in cafeteria diet obese mice.
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Related Topics
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Authors
Jonas Boström, Roine I. Olsson, Joakim Tholander, Peter J. Greasley, Erik Ryberg, Henrik Nordberg, Stephan Hjorth, Leifeng Cheng,