Abstract
Highly potent, selective, and bioavailable inhibitors of human, mouse, or rat cathepsin S are described. The key structural features combine a sulfonyl moiety attached to a large group in P2 and a small substituent in P3.
MeSH terms
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Animals
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Cathepsins / antagonists & inhibitors*
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Chemistry, Pharmaceutical / methods*
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Cysteine Proteinase Inhibitors / chemistry
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Drug Design
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Drug Evaluation, Preclinical
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Humans
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Inhibitory Concentration 50
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Mice
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Models, Chemical
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Models, Molecular
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Molecular Conformation
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Molecular Structure
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Protein Binding
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Rats
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Structure-Activity Relationship
Substances
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Cysteine Proteinase Inhibitors
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Cathepsins
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cathepsin S