Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372091 | Bioorganic & Medicinal Chemistry Letters | 2010 | 6 Pages |
Abstract
The synthesis and structure–activity relationship studies of imidazoles are described. The target compounds 6–20 represent a novel chemotype of potent and CB2/CB1 selective cannabinoid CB2 receptor antagonists/inverse agonists with very high binding efficiencies in combination with favourable log P and calculated polar surface area values. Compound 12 exhibited the highest CB2 receptor affinity (Ki = 1.03 nM) in this series, as well as the highest CB2/CB1 subtype selectivity (>9708-fold).
Graphical abstractImidazoles represent a novel chemotype of potent and selective CB2 receptor antagonists.Figure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jos H.M. Lange, Martina A.W. van der Neut, Henri C. Wals, Gijs D. Kuil, Alice J.M. Borst, Arie Mulder, Arnold P. den Hartog, Hicham Zilaout, Wouter Goutier, Herman H. van Stuivenberg, Bernard J. van Vliet,