학술논문
Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies
Document Type
Article
Author
Source
Subject
*ORGANIC synthesis
*IMIDAZOLES
*DRUG synergism
*CANNABINOIDS
*STRUCTURE-activity relationship in pharmacology
*TARGETED drug delivery
*DRUG lipophilicity
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Language
ISSN
0960-894X
Abstract
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 (K i =1.03 nM) in this series, as well as the highest CB2/CB1 subtype selectivity (>9708-fold). [Copyright &y& Elsevier]