Synthesis of 2,3-Disubstituted 1,4-Naphthoquinones as Antiplatelet Agents

✍ Scribed by Jin-Cherng Lien; Chi-Rei Wu; Mann-Jen Hour; Li-Jiau Huang; Tur-Fu Huang; Sheng-Chu Kuo

• Publisher: John Wiley and Sons
• Year: 2008
• Tongue: English
• Weight: 605 KB
• Volume: 341
• Category: Article
• ISSN: 0365-6233
• DOI: 10.1002/ardp.200800024

✦ Synopsis

Abstract

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.