Synthesis and SAR studies of benzimidazolone derivatives as histamine H3-receptor antagonists.

Qingbei Zeng,Stuart B Rosenblum,Zhaoxia Yang,Yueheng Jiang,Kevin D McCormick,Robert G Aslanian,Luli Duguma,Joseph A Kozlowski,Neng-Yang Shih,John A Hey,Robert E West,Walter A Korfmacher,Michael Berlin,Christopher W Boyce

Bioorganic & Medicinal Chemistry Letters（2013）

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摘要

A novel series of benzimidazolone-containing histamine H3-receptor antagonists were prepared and their structure–activity relationship was explored. These benzimidazolone analogs demonstrate potent H3-receptor binding affinities, no P450 enzyme inhibition, and strong H3 functional activity. Compound 1o exhibits the best overall profile with H3Ki=0.95nM and rat AUC=12.9μMh.

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关键词

H3-antagonists,Benzimidazolone,P450 inhibition

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