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ABSTRACT: 2-(Dialkylamino)chromones 4 and 4-(1-piperazinyl)coumarins 11, as well as their angular benzo-fused derivatives 1, 2 and 12, 13, respectively, were synthesized and tested in vitro for their inhibitory activity on human platelet aggregation induced in platelet-rich plasma by ADP (5.0 microM), collagen (10.0 micrograms/ml), and A 23187 (calcimycin) (20.0 microM). Among the dialkylamino substituents used, and the ring systems examined, 1-piperazinyl and 1-benzopyran or naphtho[2,1-b]pyran, respectively, resulted the most effective ones for antiplatelet activity, both in the chromone and coumarin fields. 7-Ethoxy-4-(1-piperazinyl)coumarin 11b showed the highest activity, and higher than those of all reference compounds (ASA, trifluoperazine, propranolol, and dipyridamole) towards all platelet aggregation inducers.
Il Farmaco 11/1995; 50(10):703-11.
