M. Dibraccio et al., PYRAN DERIVATIVES .19. (DIALKYLAMINO) SUBSTITUTED 1-BENZOPYRANONES AND NAPHTHOPYRANONES WITH PLATELET ANTIAGGREGATING ACTIVITY, Il Farmaco, 50(10), 1995, pp. 703-711
2-(Dialkylamino)chromones 4 and 4-(1-piperazinyl)coumarins 11, as well
as their angular benzo-fused derivatives 1, 2 and 12, 13, respectivel
y, were synthesized and tested in vitro for their inhibitory activity
on human platelet aggregation induced in platelet-rich plasma by ADP (
5.0 mu M), collagen (10.0 mu g/ml), and A 23187 (calcimycin) (20.0 mu
M). Among the dialkylamino substituents used, and the ring systems exa
mined, 1-piperazinyl and 1-benzopyran or naphtho[2,1-b]pyran, respecti
vely, resulted the most effective ones for antiplatelet activity, both
in the chromone and coumarin fields. 7-Ethoxy-4-(1-piperazinyl)coumar
in 11b showed the highest activity, and higher than those of all refer
ence compounds (ASA, trifluoperazine, propranolol, and dipyridamole) t
owards all platelet aggregation inducers.