Synthesis and antiplatelet activity of phenyl quinolones

被引：123

作者：

Huang, LJ

Hsieh, MC

Teng, CM

Lee, KH

Kuo, SC ^{[1
]}

机构：

[1] China Med Coll, Grad Inst Pharmaceut Chem, Taichung, Taiwan

[2] Natl Taiwan Univ, Coll Med, Inst Pharmacol, Taipei, Taiwan

[3] Univ N Carolina, Sch Pharm, Div Med Chem & Nat Prod, Nat Prod Lab, Chapel Hill, NC 27599 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1998年 / 6卷 / 10期

关键词：

phenyl quinolone; antiplatelet activity; platelet aggregation; arachidonic acid; antiinflammatory;

D O I：

10.1016/S0968-0896(98)00141-2

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：1657 / 1662

页数：6

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