Inhibitory effect of aryl thienyl-ketones and -thioketones on arachidonic acid-induced malondialdehyde formation in human platelets: biological data and molecular modelling.
J Enzyme Inhib
; 5(4): 281-91, 1992.
Article
em En
| MEDLINE
| ID: mdl-1285249
ABSTRACT
A series of anti-thrombotic aryl thienyl-ketones and -thioketones was assayed in vitro for their inhibitory effect on malondialdehyde (MDA) production induced by arachidonic acid in human platelets. For several compounds MDA formation was strongly inhibited indicating that the anti-platelet target was situated on the cyclooxygenase pathway. A comparison between the inhibition constant Ki and the IC50 values revealed competitive inhibition kinetics. The molecular structure of one active compound was analysed by X-ray diffraction and theoretical calculations to provide information on its electronic and lipophilic properties.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos de Sulfidrila
/
Plaquetas
/
Inibidores de Ciclo-Oxigenase
/
Ácido Araquidônico
/
Cetonas
/
Malondialdeído
Limite:
Humans
Idioma:
En
Revista:
J Enzyme Inhib
Assunto da revista:
BIOQUIMICA
Ano de publicação:
1992
Tipo de documento:
Article
País de afiliação:
França