Design, Synthesis and Biological Activity of Rigid Cannabinoid CB_1 Receptor Antagonists

概要

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The design, synthesis and biological activities of potent pyrazole-based tricyclic CB_1, receptor antagonists (2) are described. The key synthetic step involves the ring closure of the lithiated α,γ-keto ester adduct (4). The optimal nitroderivative (28) in this series exhibits a high CB_1 receptor affinity (pK_i=7.2) as well as very potent antagonistic activity (pA_2=8.8) in vitro. The regioselectivity of the pyrazole ring closure is shown to depend strongly on the aromatic substitution pattern of the applied arylhydrazine.
公益社団法人日本薬学会の論文
2002-08-01