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Novel 2-oxoamide inhibitors of human group IVA phospholipase A(2)
George Kokotos1, Stavroula Kotsovolou, David A Six
1Laboratory of Organic Chemistry, Department of Chemistry, University of Athens, Panepistimiopolis, Athens 15771, Greece. gkokotos@cc.uoa.gr
Journal of Medicinal Chemistry
|June 28, 2002
Abstract:
A novel class of potent human cytosolic phospholipase A(2) (GIVA PLA(2)) inhibitors was developed. These inhibitors were designed to contain the 2-oxoamide functionality and a free carboxyl group. Among the compounds tested, a long-chain 2-oxoamide containing L-gamma-norleucine was the most potent inhibitor, causing a 50% decrease in GIVA PLA(2) activity at 0.009 mole fraction.