548760-13-0Relevant academic research and scientific papers
Scaffold hopping, synthesis and structure-activity relationships of 5,6-diaryl-pyrazine-2-amide derivatives: A novel series of CB1 receptor antagonists
Bostroem, Jonas,Berggren, Kristina,Elebring, Thomas,Greasley, Peter J.,Wilstermann, Michael
, p. 4077 - 4084 (2008/03/12)
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 10 nM for the CB1 receptor.
2-SUBSTITUED 5, 6-DIARYL-PYRAZINE DERIVATIVES AS CB1 MODULATOR.
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Page 20; 21, (2008/06/13)
The present invention relates to 5, 6-diaryl-pyrazine-2-carboxamide and- 2-ester derivatives and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them. The compounds are cannabinoid receptor 1 (CB1) modulators.
