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

详细信息    查看全文

• 作者：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 Jr. ; Walter A. Korfmacher ; Michael Berlin ; Christopher W. Boyce
• 关键词：H3-antagonists ; Benzimidazolone ; P450 inhibition
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：1 November, 2013
• 年：2013
• 卷：23
• 期：21
• 页码：6001-6003
• 全文大小：686 K

文摘

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 ass=""boldFont"">1o exhibits the best overall profile with H₃K_i = 0.95 nM and rat AUC = 12.9 ¦ÌM h.