1469924-47-7Relevant articles and documents
Synthesis and SAR studies of benzimidazolone derivatives as histamine H3-receptor antagonists
Zeng, Qingbei,Rosenblum, Stuart B.,Yang, Zhaoxia,Jiang, Yueheng,McCormick, Kevin D.,Aslanian, Robert G.,Duguma, Luli,Kozlowski, Joseph A.,Shih, Neng-Yang,Hey, John A.,West Jr., Robert E.,Korfmacher, Walter A.,Berlin, Michael,Boyce, Christopher W.
, p. 6001 - 6003 (2013/10/22)
A novel series of benzimidazolone-containing histamine H 3-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 = 0.95 nM and rat AUC = 12.9 μM h.
