Design, synthesis and biological evaluation of CB1 cannabinoid receptor ligands derived from the 1,5-diarylpyrazole
GuoGang Tu1, Fang Xiong, HuiMing Huang
1Department of Medicinal Chemistry, NanChang University School of Pharmaceutical Science, NanChang, PR China.
Journal of Enzyme Inhibition and Medicinal Chemistry
|June 23, 2010
Abstract:
The CB1 receptor belongs to the G-protein-coupled receptor superfamily. CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. In this study, we report the synthesis and in vitro binding affinity assay of some 1,5-diarylpyrazole scaffold compounds. The binding results showed that some of the target compounds had an excellent potency toward the CB1 receptor with IC₅₀ values lying at the nanomole level.
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