1.
Bioorg Med Chem Lett
; 16(10): 2729-33, 2006 May 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-16504501
RESUMEN
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.
Asunto(s)
Inhibidores Enzimáticos/farmacología , Naftalenos/farmacología , Propionatos/farmacología , Tretinoina/metabolismo , Cromatografía Líquida de Alta Presión , Inhibidores Enzimáticos del Citocromo P-450 , Sistema Enzimático del Citocromo P-450 , Inhibidores Enzimáticos/farmacocinética , Semivida , Espectrometría de Masas , Naftalenos/farmacocinética , Propionatos/farmacocinética , Ácido Retinoico 4-Hidroxilasa , Tretinoina/antagonistas & inhibidores
2.
Bioorg Med Chem Lett
; 15(6): 1669-73, 2005 Mar 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-15745819
RESUMEN
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).