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.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Amides / chemical synthesis*
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Amides / chemistry
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Amides / pharmacology
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Group IV Phospholipases A2
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Humans
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Magnetic Resonance Spectroscopy
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Norleucine / analogs & derivatives*
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Norleucine / chemical synthesis*
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Norleucine / chemistry
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Phospholipases A / antagonists & inhibitors*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Amides
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Enzyme Inhibitors
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Norleucine
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Phospholipases A
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Group IV Phospholipases A2
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PLA2G4A protein, human