Novel imidazole-based histamine H3 antagonists

A novel series of imidazole containing histamine H3 receptor ligands were investigated and found to be potent functional antagonists. After improving the stability of these molecules towards liver microsomes, these compounds were found to have no appreciable affinity for CYP P450s. Subsequent in vivo experiments showed significant brain uptake of (4-chloro-phenyl)-[2-(1-isopropyl-piperidin-4-ylmethoxy)-3-methyl-3H-imidazol-4-yl]-methanone 22.

A novel series of imidazole containing histamine H3 receptor ligands were Investigated and found to be potent functional antagonists with appreciable brain uptake.Figure optionsDownload as PowerPoint slide