13515-07-6Relevant articles and documents
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.