1.
Bioorg Med Chem Lett
; 16(10): 2729-33, 2006 May 15.
Article
in English
| MEDLINE
| ID: mdl-16504501
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.
Subject(s)
Enzyme Inhibitors/pharmacology , Naphthalenes/pharmacology , Propionates/pharmacology , Tretinoin/metabolism , 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
2.
Bioorg Med Chem Lett
; 15(6): 1669-73, 2005 Mar 15.
Article
in English
| MEDLINE
| ID: mdl-15745819
ABSTRACT
A series of [2-imidazol-1-yl-2-(6-alkoxy-naphthalen-2-yl)-1-methyl-ethyl]-dimethyl-amines were designed and synthesized as CYP26 inhibitors, serving as retinoic acid metabolic blocking agents (RAMBA's).