Abstract
Pyridone-based peptidomimetic inhibitors of recombinant human Interleukin-1 beta-converting enzyme (ICE, caspase-1) with an aminomethylene ketone activating group in the P1' position are described. Several analogues with sub-nanomolar Ki's versus ICE and improved aqueous solubility are reported.
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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Caspase Inhibitors*
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Cysteine Proteinase Inhibitors / chemical synthesis*
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Cysteine Proteinase Inhibitors / chemistry
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Cysteine Proteinase Inhibitors / pharmacology
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Humans
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Kinetics
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Molecular Structure
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Pyridones / chemical synthesis*
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Pyridones / chemistry
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Pyridones / pharmacology
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Recombinant Proteins / antagonists & inhibitors
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Solubility
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Structure-Activity Relationship
Substances
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Amides
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Caspase Inhibitors
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Cysteine Proteinase Inhibitors
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Pyridones
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Recombinant Proteins