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

Wu, Yiran
Chen, Zheng
Liu, Ying
Yu, Lanlan
Zhou, Lu
Yang, Suijia
Lai, Luhua

Open link

Publication date

January 2011

DOI

10.1016/j.bmc.2011.04.039

Publisher

生物有机化学与医药化学

ISSN

0968-0896

Journal

issn:0968-0896

Citation count (estimate)

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 IC50 value for the best compound 3o was 1.5 mu M. The structure-inhibition-activity relationships of the compounds were studied using molecular docking. Crown Copyright (C) 2011 Published by Elsevier Ltd. All rights reserved.Biochemistry & Molecular BiologyChemistry, MedicinalChemistry, OrganicSCI(E)PubMed4ARTICLE113361-33661