Scaffold hopping, synthesis and structure–activity relationships of 5, 6-diaryl-pyrazine-2-amide derivatives: a novel series of CB1 receptor antagonists
J Boström, K Berggren, T Elebring, PJ Greasley…
文献索引：Bostroem, Jonas; Berggren, Kristina; Elebring, Thomas; Greasley, Peter J.; Wilstermann, Michael Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 12 p. 4077 - 4084
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 ...
