Abstract
Simplified analogs of YM-26734, a known inhibitor of secreted phospholipase A(2) (sPLA(2)) group IIA, were synthesized and found to also display potent inhibition at low nanomolar concentrations. Analogs were based on the didodecanoylphloroglucinol portion of YM-26734 which contains the predicted active site calcium binding group.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Calcium / chemistry
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Catalytic Domain
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Chemistry, Pharmaceutical / methods*
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Chromans / antagonists & inhibitors*
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Chromans / pharmacology*
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Drug Design
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Group II Phospholipases A2 / antagonists & inhibitors*
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Humans
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Indoles / chemistry
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Inhibitory Concentration 50
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Mice
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Models, Theoretical
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Phenols / antagonists & inhibitors*
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Phenols / pharmacology*
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Protein Binding
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Rats
Substances
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Chromans
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Indoles
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Phenols
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YM 26734
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indole
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Group II Phospholipases A2
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Calcium