Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375682 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
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.
Graphical abstractA novel series of imidazole containing histamine H3 receptor ligands were Investigated and found to be potent functional antagonists with appreciable brain uptake.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jill A. Jablonowski, Kiev S. Ly, Michael Bogenstaetter, Curt A. Dvorak, Jamin D. Boggs, Lisa K. Dvorak, Brian Lord, Kirsten L. Miller, Curt Mazur, Sandy J. Wilson, Timothy W. Lovenberg, Nicholas I. Carruthers,