Synthesis and antiplatelet activity of phenyl quinolones
Synthesis and antiplatelet activity of phenyl quinolones
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DOI：
10.1016/s0968-0896(98)00141-2
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发表时间：
1998-10-01
影响因子：
3.5
通讯作者：
Kuo, SC
中科院分区：
文献类型：
--
作者：
Huang, LJ;Hsieh, MC;Kuo, SC
在我们寻找新型抗血小板药物的过程中，合成了七种苯基喹诺酮位置异构体。初步筛选证实它们对花生四烯酸（AA）诱导的血小板聚集有抑制作用。改变苯基的取代位置对这些异构体的抗血小板活性具有深远的影响。 3-苯基-4-喹诺酮显示出最大的效力并且优于吲哚美辛，尽管这两种结构有很大不同。 3-苯基-4-喹诺酮的作用机制和药理作用目前正在研究中。 (C) 1998 Elsevier Science Ltd. 保留所有权利。
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. (C) 1998 Elsevier Science Ltd. All rights reserved.