2-Heteroaryl 2-substituted phenylketone derivatives and their inhibitory activity on platelet aggregation.
J Pharm Pharmacol
; 47(9): 762-7, 1995 Sep.
Article
em En
| MEDLINE
| ID: mdl-8583390
ABSTRACT
R 68070 and CV-4151 are two compounds possessing both thromboxane synthetase inhibitory activity and thromboxane receptor antagonist properties. 2-Heteroaryl 2-substituted phenylketone derivatives with a partial structural similarity to R 68070 and CV-4151, i.e. possessing a phenyl and a heteroaryl moiety, have been prepared and found to have antiplatelet activity. The compound 2-thienyl 2'-hydroxyphenyl ketone (4) was shown to completely inhibit platelet aggregation induced by arachidonic acid at a concentration of 5.0 microM. Structure-activity analysis indicated that the presence of a ketone group is an important requirement for this inhibitory activity. An o-hydroxyl substitution on the phenyl ring, and a 2-thienyl of heteroaryl ring might increase inhibitory activity.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ácidos Pentanoicos
/
Piridinas
/
Tromboxano-A Sintase
/
Ácidos Graxos Monoinsaturados
/
Inibidores da Agregação Plaquetária
/
Fibrinolíticos
Limite:
Animals
Idioma:
En
Revista:
J Pharm Pharmacol
Ano de publicação:
1995
Tipo de documento:
Article
País de afiliação:
China