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3-[6-(2-Dimethylamino-1-imidazol-1-yl-butyl)-naphthalen-2-yloxy]-2,2-dimethyl-propionic acid as a highly potent and selective retinoic acid metabolic blocking agent.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 May 15; Vol. 16 (10), pp. 2729-33. Date of Electronic Publication: 2006 Feb 28. - Publication Year :
- 2006
-
Abstract
- 3-[6-(2-Dimethylamino-1-imidazol-1-yl-butyl)-naphthalen-2-yloxy]-2,2-dimethyl-propionic acid and analogs were designed and synthesized as highly potent and selective CYP26 inhibitors, serving as retinoic acid metabolic blocking agents (RAMBAs), with demonstrated in vivo efficacy to increase the half-life of exogenous atRA.
- Subjects :
- Chromatography, High Pressure Liquid
Cytochrome P-450 Enzyme Inhibitors
Cytochrome P-450 Enzyme System
Enzyme Inhibitors pharmacokinetics
Half-Life
Mass Spectrometry
Naphthalenes pharmacokinetics
Propionates pharmacokinetics
Retinoic Acid 4-Hydroxylase
Tretinoin antagonists & inhibitors
Enzyme Inhibitors pharmacology
Naphthalenes pharmacology
Propionates pharmacology
Tretinoin metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 16
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 16504501
- Full Text :
- https://doi.org/10.1016/j.bmcl.2006.02.020