Synthesis and structure–activity relationships of 2-(1,4′-bipiperidin-1′-yl)thiazolopyridine as H₃ receptor antagonists

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• 作者：Ashwin U. Rao ; An ; an Palani ; Xiao Chen ; Ying Huang ; Robert G. Aslanian ; Robert E. West Jr. ; Shirley M. Williams ; Ren-Long Wu ; JoyceHwa ; Christopher Sondey ; Jean Lachowicz
• 关键词：Histamine ; H3 ; 2-(1 ; 4′ ; -Bipiperidin-1′ ; -yl)thiazolopyridine
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：1 November 2009
• 年：2009
• 卷：19
• 期：21
• 页码：6176-6180
• 全文大小：1375 K

文摘

A series of 2-(1,4′-bipiperidine-1′-yl)thiazolopyridines was synthesized and evaluated as a new lead of non-imidazole histamine H₃ receptor antagonists. Introduction of diversity at the 6-position of the pyridine ring was designed to enhance in vitro potency and decrease hERG activity. The structure–activity relationships for these new thiazolopyridine antagonists are discussed.