Lien Jin-Cherng, Wu Chi-Rei, Hour Mann-Jen, Huang Li-Jiau, Huang Tur-Fu, Kuo Sheng-Chu
Graduate Institute of Chinese Pharmaceutical Sciences, Taichung, Taiwan, R.O.C.
Arch Pharm (Weinheim). 2008 Oct;341(10):639-44. doi: 10.1002/ardp.200800024.
In continuing search for novel antiplatelet agents, the highly potent agent 2-chloro-3-methoxycarbonylethylcarboxamido-1,4-naphthoquinone 2 was selected as lead compound. Structure-activity relationships in this series were examined. Some of these compounds showed significant antiplatelet activities. Further studies on the action mechanism showed that 2-acetamido-3-chloro-1,4-naphthoquinone 4 has a direct inhibitory action on cytosolic phospholipase A(2) (cPLA(2)) activity in platelets.
在持续寻找新型抗血小板药物的过程中，高效药物2-氯-3-甲氧羰基乙基甲酰胺基-1,4-萘醌2被选为先导化合物。研究了该系列的构效关系。其中一些化合物表现出显著的抗血小板活性。对作用机制的进一步研究表明，2-乙酰氨基-3-氯-1,4-萘醌4对血小板中的胞质磷脂酶A(2)（cPLA(2)）活性具有直接抑制作用。
