title: Synthesis and antiplatelet activity of phenyl quinolones.
abstract: In our search for novel antiplatelet agents, seven positional phenyl quinolone isomers were synthesized. Preliminary screening confirmed their inhibitory effects against arachidonic acid (AA)-induced platelet aggregation. Varying the substitutional position of the phenyl group had a profound effect on the antiplatelet activity of these isomers. 3-Phenyl-4-quinolone showed the greatest potency and was superior to indomethacin, although the two structures are quite different. The mechanism and pharmacological action of 3-phenyl-4-quinolone are currently under investigation.
authors.affiliation: Graduate Institute of Pharmaceutical Chemistry, China Medical College, Taichung, Taiwan.
authors.forename: L J
authors.initials: LJ
authors.lastname: Huang
authors.forename: M C
authors.initials: MC
authors.lastname: Hsieh
authors.forename: C M
authors.initials: CM
authors.lastname: Teng
authors.forename: K H
authors.initials: KH
authors.lastname: Lee
authors.forename: S C
authors.initials: SC
authors.lastname: Kuo
mesh_terms: D000818:Animals; D007536:Isomerism; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011817:Rabbits; D013329:Structure-Activity Relationship
chemical_list: C116513:3-phenyl-2-quinolone; D010975:Platelet Aggregation Inhibitors; D015363:Quinolones; C084179:2-phenyl-4-oxohydroquinoline