Abstract
Two novel 8,6-fused bicyclic peptidomimetic ring systems were synthesized utilizing olefin metathesis as the key reaction for the formation of the eight-membered ring. Both peptidomimetic scaffolds were further elaborated into potent ICE inhibitors, with numerous compounds exhibiting caspase-1 IC(50)s less than 10nM.
MeSH terms
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Biomimetics*
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Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis
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Bridged Bicyclo Compounds, Heterocyclic / pharmacology*
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Caspase Inhibitors*
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology*
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Humans
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Indicators and Reagents
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Models, Molecular
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Molecular Conformation
Substances
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Bridged Bicyclo Compounds, Heterocyclic
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Caspase Inhibitors
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Enzyme Inhibitors
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Indicators and Reagents