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Research Article

Inhibitory Effect of Aryl Thienyl-Ketones and - Thioketones on Arachidonic Acid-induced Malondialdehyde Formation in Human Platelets: Biological Data and Molecular Modelling

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Pages 281-291 | Received 06 Jun 1991, Published online: 27 Sep 2008
 

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 K1 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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