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

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.

Graphical abstractA series of 2-(1,4′-bipiperidine-1′-yl)thiazolopyridines was discovered as novel non-imidazole histamine H3 receptor antagonists. The synthesis and structure–activity relationships for these new thiazolopyridine antagonists are described.Figure optionsDownload full-size imageDownload as PowerPoint slide