Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A₂ Type X (sPLA₂-X) Inhibitors

Abstract

In order to assess the potential of sPLA2-X as a therapeutic target for atherosclerosis, novel sPLA2 inhibitors with improved type X selectivity are required. To achieve the objective of identifying such compounds, we embarked on a lead generation effort that resulted in the identification of a novel series of indole-2-carboxamides as selective sPLA2-X inhibitors with excellent potential for further optimization.