Synthesis of 2,3-disubstituted 1,4-naphthoquinones as antiplatelet agents

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. Structureactivity 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 A2 (cPLA2) activity in platelets. © 2008 Wiley-VCH Verlag GmbH & Co. KGaA.