Synthesis and antiplatelet activity of phenyl quinolones.
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.
Huang
L J
LJ
Graduate Institute of Pharmaceutical Chemistry, China Medical College, Taichung, Taiwan.
Hsieh
M C
MC
Teng
C M
CM
Lee
K H
KH
Kuo
S C
SC
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
C116513:3-phenyl-2-quinolone; D010975:Platelet Aggregation Inhibitors; D015363:Quinolones; C084179:2-phenyl-4-oxohydroquinoline