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Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Feb 15; Vol. 16 (4), pp. 989-94. Date of Electronic Publication: 2005 Nov 15. - Publication Year :
- 2006
-
Abstract
- A novel series of histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine template displaying low CYP2D6 and CYP3A4 inhibitory profiles has been identified. Structural features responsible for the reduction of P450 activity, a typical liability of 4-substituted imidazoles, have been established.
- Subjects :
- Animals
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Guinea Pigs
Haplorhini
Histamine Antagonists chemical synthesis
Histamine Antagonists chemistry
Humans
Imidazoles chemical synthesis
Imidazoles chemistry
Molecular Structure
Piperidines chemical synthesis
Piperidines chemistry
Rats
Structure-Activity Relationship
Tissue Distribution
Cytochrome P-450 Enzyme Inhibitors
Enzyme Inhibitors pharmacology
Histamine Antagonists pharmacology
Imidazoles pharmacology
Piperidines pharmacology
Receptors, Histamine H3 drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 16
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 16297617
- Full Text :
- https://doi.org/10.1016/j.bmcl.2005.10.087