Scaffold hopping, synthesis and structure-activity relationships of 5,6-diaryl-pyrazine-2-amide derivatives: a novel series of CB1 receptor antagonists.
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Bostrom J, Berggren K, Elebring T, Greasley PJ, Wilstermann M
Scaffold hopping, synthesis and structure-activity relationships of 5,6-diaryl-pyrazine-2-amide derivatives: a novel series of CB1 receptor antagonists.
Bioorg Med Chem. 2007 Jun 15;15(12):4077-84. Epub 2007 Mar 30.
- PubMed ID
- 17433696 [ View in PubMed]
- Abstract
A scaffold hopping approach has been exploited to design a novel class of cannabinoid (CB1) receptor antagonists for the treatment of obesity. On the basis of shape-complementarity and synthetic feasibility the central fragment, a methylpyrazole, in Rimonabant was replaced by a pyrazine. The synthesis and CB1 antagonistic activities of a new series of 5,6-diaryl-pyrazine-2-amide derivatives are described. Several compounds showed antagonist potency below 10nM for the CB1 receptor.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Rimonabant Cannabinoid receptor 1 IC 50 (nM) 3 7.4 30 Details Rimonabant Cannabinoid receptor 1 IC 50 (nM) 3 N/A N/A Details