Synthesis and pharmacological evaluation of 2,3-dialkylindoles, "in vitro" inhibitors of thrombin-induced platelet aggregation
Arcari, M.; Aveta, R.; Brandt, A.; Cecchetelli, L.; Corsi, G.B.; Solinas, F.
Farmaco 47(4): 405-425
1992
ISSN/ISBN: 0014-827X PMID: 1388590 Document Number: 397479
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.