Bicyclic and tricyclic heterocycle derivatives as histamine H₃ receptor antagonists for the treatment of obesity

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• 作者：Manuel de Lera Ruiz ; Junying Zheng ; Michael Y. Berlin ; Kevin D. McCormick ; Robert G. Aslanian ; Robert West ; Joyce Hwa ; Jean Lachowicz ; Margaret van Heek
• 关键词：Histamine ; H3 antagonists
• 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：6004-6009
• 全文大小：1952 K

文摘

A novel series of non-imidazole bicyclic and tricyclic histamine H₃ receptor antagonists has been discovered. Compound 17 was identified as a centrally penetrant molecule with high receptor occupancy which demonstrates robust oral activity in rodent models of obesity. In addition compound 17 possesses clean CYP and hERG profiles and shows no behavioral changes in the Irwin test.