… selective secretory phospholipase A 2 inhibitors. Part 5: Synthesis and biological activity of 1-alkyl-4-[4, 5-dihydro-1, 2, 4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4′-yl ( …

…, M Touaibia, N Meddad-Belhabich, A Djimdé…

Index: Boukli, Latifa; Touaibia, Mohamed; Meddad-Belhabich, Nadia; Djimde, Atime; Park, Chang-Ha; Kim, Jung-Joo; Yoon, Joo-Hyoung; Lamouri, Aazdine; Heymans, Francoise Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 3 p. 1242 - 1253

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Citation Number: 14

Abstract

Among the different PLA2s identified to date, the group IIA secretory PLA2 (sPLA2 GIIA) is implied in diverse pathological conditions. In this work we describe the synthesis, inhibitory activities, and structure–activity relationships (SAR) of a new class of substituted piperazine derivatives. The in vitro fluorimetric assay using two groups of enzymes, GIB and GIIA, revealed several compounds as highly potent inhibitors (IC50= 0.1 μM). The in vivo ...