Quinoline-4-methyl esters as human nonpancreatic secretory phospholipase A 2 inhibitors

Y Wu, Z Chen, Y Liu, L Yu, L Zhou, S Yang…

Index: Wu, Yiran; Chen, Zheng; Liu, Ying; Yu, Lanlan; Zhou, Lu; Yang, Suijia; Lai, Luhua Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 11 p. 3361 - 3366

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Citation Number: 6

Abstract

Abstract A series of novel fused heterocycle methyl esters were designed and synthesized as human nonpancreatic secretory phospholipase A 2 (hnps-PLA 2) competitive inhibitors. Among the 22 synthesized compounds, 17 quinoline-4-methyl esters displayed hnps-PLA 2 inhibition activity in the in vitro bioassay. The IC 50 value for the best compound 3o was 1.5 μM. The structure-inhibition–activity relationships of the compounds were studied using ...