Quinoline-4-methyl esters as human nonpancreatic secretory phospholipase A2 inhibitors
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Add time:08/23/2019 Source:sciencedirect.com
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.
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