Abstract
We describe herein the synthesis and biological evaluation of a series of tripeptidyl alpha-ketoamides as human rhinovirus (HRV) 3C protease inhibitors. The most potent inhibitor discussed in this manuscript, 4I, exhibited impressive enzyme inhibitory activity as well as antiviral activity against HRV-14.
MeSH terms
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3C Viral Proteases
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Amides / chemical synthesis*
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Amides / chemistry
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Amides / pharmacology*
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Cysteine Endopeptidases
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Drug Evaluation, Preclinical
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Humans
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Protease Inhibitors / chemical synthesis*
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Protease Inhibitors / chemistry
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Protease Inhibitors / pharmacology*
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Structure-Activity Relationship
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Viral Proteins / antagonists & inhibitors*
Substances
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Amides
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Protease Inhibitors
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Viral Proteins
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Cysteine Endopeptidases
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3C Viral Proteases