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Bioorg Med Chem. 2007 Jun 15;15(12):4077-84. Epub 2007 Mar 30.

Scaffold hopping, synthesis and structure-activity relationships of 5,6-diaryl-pyrazine-2-amide derivatives: a novel series of CB1 receptor antagonists.

Author information

1
Lead Generation Department, AstraZeneca R&D Mölndal, S-431 83 Mölndal, Sweden. jonas.bostrom@astrazeneca.com

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.

PMID:
17433696
DOI:
10.1016/j.bmc.2007.03.075
[Indexed for MEDLINE]

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