Small-molecular inhibitors of Ca²âº-induced mitochondrial permeability transition (MPT) derived from muscle relaxant dantrolene.
Bioorg Med Chem
; 20(21): 6384-93, 2012 Nov 01.
Article
em En
| MEDLINE
| ID: mdl-23026083
ABSTRACT
A structure consisting of substituted hydantoin linked to a 5-(halophenyl)furan-2-yl group via an amide bond was identified as a promising scaffold for development of low-molecular-weight therapeutic agents to treat vascular dysfunction, including ischemia/reperfusion injury. Among the compounds synthesized, 5-(3,5-dichlorophenyl)-N-{2,4-dioxo-3-[(pyridin-3-yl)methyl]imidazolidin-1-yl}-2-furamide (17) possessed the most potent inhibitory activity against Ca(2+)-induced mitochondrial swelling. The structural development, synthesis and structure-activity relationship of these compounds are described.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Cálcio
/
Dantroleno
/
Proteínas de Transporte da Membrana Mitocondrial
/
Bibliotecas de Moléculas Pequenas
/
Relaxamento Muscular
Tipo de estudo:
Prognostic_studies
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Ano de publicação:
2012
Tipo de documento:
Article