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Bioorg Med Chem Lett. 2010 Feb 1;20(3):1084-9. doi: 10.1016/j.bmcl.2009.12.032. Epub 2009 Dec 11.

Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies.

Author information

1
Solvay Pharmaceuticals, Research Laboratories, CJ van Houtenlaan 36, 1381 CP Weesp, The Netherlands. jos.lange@solvay.com

Abstract

The synthesis and structure-activity relationship studies of imidazoles are described. The target compounds 6-20 represent a novel chemotype of potent and CB(2)/CB(1) selective cannabinoid CB(2) receptor antagonists/inverse agonists with very high binding efficiencies in combination with favourable logP and calculated polar surface area values. Compound 12 exhibited the highest CB(2) receptor affinity (K(i)=1.03 nM) in this series, as well as the highest CB(2)/CB(1) subtype selectivity (>9708-fold).

PMID:
20031412
DOI:
10.1016/j.bmcl.2009.12.032
[Indexed for MEDLINE]

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