1H-pyrazolo[2,3-d][1,2,4]triazine-3,7-diones as a new class of human leukocyte elastase inhibitors.
Arzneimittelforschung
; 49(12): 997-1000, 1999 Dec.
Article
em En
| MEDLINE
| ID: mdl-10635444
ABSTRACT
A novel series of 1H-2-phenyl-substituted-pyrazolo[2,3-d][1,2,4]triazine-3,7-diones (3a-g) as potential inhibitors of Human Leukocyte Elastase (HLE) are reported, the acyl-pyrazole being probably involved in the inhibition mechanism of the serino-protease enzymes. The most potent inhibitor both in vivo and in vitro was 2-o-methoxyphenyl-5-methyl-6-nitro-pyrazolo[2,3-d][1,2,4]triazine-3,7-di one (3e), which significantly suppressed the HLE-induced pulmonary injury in rats when administered orally (100 mg/kg, 3 h prior to HLE administration.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirazóis
/
Tiazinas
/
Elastase de Leucócito
/
Inibidores Enzimáticos
Limite:
Animals
/
Humans
/
Male
Idioma:
En
Revista:
Arzneimittelforschung
Ano de publicação:
1999
Tipo de documento:
Article