Pyran derivatives XIX. (Dialkylamino) substituted 1-benzopyranones and naphthopyranones with platelet antiaggregating activity.
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.
Di Braccio
M
M
Istituto di Scienze Farmaceutiche dell'Università, Genova, Italy.
Roma
G
G
Leoncini
G
G
Poggi
M
M
D003374:Coumarins / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D003374:Coumarins; D010975:Platelet Aggregation Inhibitors