Quinoline-4-methyl esters as human nonpancreatic secretory phospholipase A2 inhibitors

A series of novel fused heterocycle methyl esters were designed and synthesized as human nonpancreatic secretory phospholipase A2 (hnps-PLA2) competitive inhibitors. Among the 22 synthesized compounds, 17 quinoline-4-methyl esters displayed hnps-PLA2 inhibition activity in the in vitro bioassay. The IC50 value for the best compound 3o was 1.5 μM. The structure-inhibition–activity relationships of the compounds were studied using molecular docking.

Figure optionsDownload as PowerPoint slide