Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376548 | Bioorganic & Medicinal Chemistry Letters | 2008 | 6 Pages |
Abstract
Sulfamoyl benzamides were identified as a novel series of cannabinoid receptor ligands. Starting from a screening hit 8 that had modest affinity for the cannabinoid CB2 receptor, a parallel synthesis approach and initial SAR are described, leading to compound 27 with 120-fold functional selectivity for the CB2 receptor. This compound produced robust antiallodynic activity in rodent models of postoperative pain and neuropathic pain without traditional cannabinergic side effects.
Graphical abstractA series of novel sulfamoyl benzamide cannabinoid ligands was synthesized and their biological activity determined.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Karin Worm, Q. Jean Zhou, Christopher T. Saeui, Rosalyn C. Green, Joel A. Cassel, Gabriel J. Stabley, Robert N. DeHaven, Nathalie Conway-James, Christopher J. LaBuda, Michael Koblish, Patrick J. Little, Roland E. Dolle,