Effect of 2,4-disubstituted thiazol-5yl-aminoketones on inflammation. In vitro and in vivo biological studies: a structure-activity approach.
Res Commun Mol Pathol Pharmacol
; 96(3): 307-18, 1997 Jun.
Article
em En
| MEDLINE
| ID: mdl-9261890
ABSTRACT
Some modified novel thiazol-5yl-aminoketones were evaluated for their anti-inflammatory, analgesic and antiproteolytic activities. Their inhibitory activity on 12-lipoxygenase (12-LO) and beta-glucuronidase in vitro was estimated. Their interaction with the stable free radical 1,1-diphenyl-2-picrylhydrazyl (DPPH) and their RM values were also determined. For two of them, the effect on zoxazolamine-induced paralysis after a prolonged treatment was determined. The duration of paralysis for the same compounds, (only one administration, one before zoxazolamine injection) was recorded too. The 2-amino substituted derivatives seem to be more potent in comparison with the 2-phenyl. The tested compounds were found to influence proteolysis but not the activities at beta-glucuronidase and 12-LO. Their interaction with DPPH was mild. Compound 2 seems to modify the activity of the hepatic drug metabolizing enzymes. In conclusion, their activity is related to certain structural characteristics.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Anti-Inflamatórios não Esteroides
/
Inibidores Enzimáticos
/
Analgésicos
/
Cetonas
Limite:
Animals
Idioma:
En
Revista:
Res Commun Mol Pathol Pharmacol
Assunto da revista:
BIOLOGIA MOLECULAR
/
FARMACOLOGIA
/
PATOLOGIA
Ano de publicação:
1997
Tipo de documento:
Article
País de afiliação:
Grécia