Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies |
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| Authors: | Jos HM Lange Martina AW van der Neut Henri C Wals Gijs D Kuil Alice JM Borst Arie Mulder Arnold P den Hartog Hicham Zilaout Wouter Goutier Herman H van Stuivenberg Bernard J van Vliet |
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| Institution: | Solvay Pharmaceuticals, Research Laboratories, C. J. van Houtenlaan 36, 1381 CP Weesp, The Netherlands |
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| 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). |
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