Huang L J, Hsieh M C, Teng C M, Lee K H, Kuo S C
Graduate Institute of Pharmaceutical Chemistry, China Medical College, Taichung, Taiwan.
Bioorg Med Chem. 1998 Oct;6(10):1657-62. doi: 10.1016/s0968-0896(98)00141-2.
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.
在寻找新型抗血小板药物的过程中，合成了七种位置不同的苯基喹诺酮异构体。初步筛选证实了它们对花生四烯酸（AA）诱导的血小板聚集具有抑制作用。改变苯基的取代位置对这些异构体的抗血小板活性有深远影响。3-苯基-4-喹诺酮表现出最大的效力，并且优于吲哚美辛，尽管这两种结构有很大差异。目前正在研究3-苯基-4-喹诺酮的作用机制和药理作用。
