SYNTHESIS AND ANTIPLATELET ACTIVITY OF PHENYL QUINOLONES

In our search for novel antiplatelet agents, seven positional phenyl q uinolone isomers were synthesized. Preliminary screening confirmed the ir inhibitory effects against arachidonic acid (AA)-induced platelet a ggregation. Varying the substitutional position of the phenyl group ha d a profound effect on the antiplatelet activity of these isomers. 3-P henyl-4-quinolone showed the greatest potency and was superior to indo methacin, although the two structures are quite different. The mechani sm and pharmacological action of 3-phenyl-4-quinolone are currently un der investigation. (C) 1998 Elsevier Science Ltd. All rights reserved.