Inhibition of human sputum elastase by 7-substituted 5-methyl-2-isopropylamino-4H-3,1-benzoxazin-4-ones.
Biochem Pharmacol
; 48(2): 426-8, 1994 Jul 19.
Article
en En
| MEDLINE
| ID: mdl-8053939
ABSTRACT
7-Substituted 5-methyl-2-isopropylamino-4H-3,1-benzoxazin-4-ones (BOZNs) were prepared and tested as inhibitors of human sputum elastase (HSE). The BOZNs with certain amino acid residues at the 7-position proved to be potent inhibitors of HSE. Some of the compounds also showed a high selectivity for HSE versus chymotrypsin. In a hamster model in which acute injury was induced by intratracheal administration of HSE (1.0 mg/kg), these compounds, when administered intratracheally (1.0 mg/kg) either 30 or even 240 min before challenge with HSE, significantly suppressed pulmonary hemorrhage. These findings suggest that 7-substitution of BOZN by amino acid residues can produce strong and HSE-specific inhibitors, with potential use in elastase-mediated disorders.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Oxazinas
/
Esputo
/
Elastasa Pancreática
/
Leucocitos
Tipo de estudio:
Prognostic_studies
Límite:
Animals
Idioma:
En
Revista:
Biochem Pharmacol
Año:
1994
Tipo del documento:
Article
País de afiliación:
Japón