Benzimidazole-substituted (3-phenoxypropyl)amines as histamine H3 receptor ligands

A series of non-imidazole histamine H3 receptor antagonists based on the (3-phenoxypropyl)amine motif, which is a common pharmacophore for H3 antagonists, has been identified. A preliminary SAR study around the amine moiety has identified 8a as a potent H3 antagonist possessing a good pharmacokinetic profile in the rat.

A series of non-imidazole histamine H3 receptor antagonists based on the (3-phenoxypropyl)amine motif have been identified. Compound 8a displays a good pharmacokinetic profile in the rat.Figure optionsDownload as PowerPoint slide