633310-75-5Relevant academic research and scientific papers
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.
1-(4-PIPERIDINYL) BENZIMIDAZOLONES AS HISTAMINE H3 ANTAGONISTS
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Page 53, (2010/02/04)
Disclosed are histamine H3 antagonists of the formula (I) wherein R1 is benzimidazolone derivative, M1 and M2 are optionally substituted carbon or nitrogen, R2 includes optionally substituted aryl or heteroaryl, and the remaining variables are as defined
