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Synthesis and pharmacological evaluation of 2,3-dialkylindoles, "in vitro" inhibitors of thrombin-induced platelet aggregation.
Authors:M Arcari  R Aveta  A Brandt  L Cecchetelli  G B Corsi  F Solinas
Affiliation:Istituto Biochimico Italiano, IBI Sud, Research Laboratories, Aprilia, (LT).
Abstract:A series of 2,3-dialkylindoles (1-5) have been prepared and tested as antithrombotic agents. The whole class showed in vitro interesting activity in the inhibition of thrombin-induced aggregation. Among these compounds some ones showed activity comparable to standards also in the inhibition of collagen-induced aggregation. Owing to a very fast metabolic degradation through a beta-oxidative mechanism, a drastic decrease of activity in several tests ex vivo or in vivo was observed.
Keywords:
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