Peer-reviewed veterinary case report
Novel thioamide derivatives as neutral CB1 receptor antagonists.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2010
- Authors:
- Boström, Jonas et al.
- Affiliation:
- Lead Generation Department
- Species:
- rodent
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 10nM), but also showed improved solubility. In addition, the neutral antagonist 2c significantly reduced body weight in cafeteria diet obese mice.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/20005704/