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    J Med Chem. 2002 Jul 4;45(14):2891-3.

    Novel 2-oxoamide inhibitors of human group IVA phospholipase A(2).

    Kokotos G, Kotsovolou S, Six DA, Constantinou-Kokotou V, Beltzner CC, Dennis EA.

    Laboratory of Organic Chemistry, Department of Chemistry, University of Athens, Panepistimiopolis, Athens 15771, Greece. gkokotos@cc.uoa.gr

    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.

    PMID: 12086476 [PubMed - indexed for MEDLINE]

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