Abstract
This paper details exploration of a class of triazole-based cathepsin S inhibitors originally reported by Ellman and co-workers. SAR studies involving modifications across the whole inhibitor provide a perspective on the strengths and weaknesses of this class of inhibitors. In addition, we put the unique characteristics of this class of compounds into perspective with other classes of cathepsin S inhibitors.
Copyright © 2012 Elsevier Ltd. All rights reserved.
MeSH terms
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Amides / chemistry*
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Cathepsins / antagonists & inhibitors*
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Cathepsins / metabolism
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Half-Life
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Humans
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Microsomes, Liver / metabolism
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Protease Inhibitors / chemical synthesis
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Protease Inhibitors / chemistry*
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Protease Inhibitors / pharmacokinetics
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Protein Binding
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Structure-Activity Relationship
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Thiophenes / chemical synthesis
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Thiophenes / chemistry*
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Thiophenes / pharmacokinetics
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Triazoles / chemical synthesis
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Triazoles / chemistry*
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Triazoles / pharmacokinetics
Substances
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Amides
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Protease Inhibitors
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Thiophenes
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Triazoles
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Cathepsins
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cathepsin S