Abstract
A series of dipeptide nitriles with a thienyl alanine in P2 were identified as potent and selective cathepsin C inhibitors. Incorporation of a substituted cyclopropyl moiety in P1 effectively protects these derivatives against hydrolase activity in whole blood.
MeSH terms
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Animals
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Cathepsin C / antagonists & inhibitors*
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Cathepsin C / metabolism*
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Cell Line
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Dipeptides / blood
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Dipeptides / chemical synthesis
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Dipeptides / chemistry*
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Dipeptides / pharmacology*
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Humans
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Nitriles / blood
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Nitriles / chemical synthesis
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Nitriles / chemistry*
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Nitriles / pharmacology*
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Rats
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Structure-Activity Relationship
Substances
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Dipeptides
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Nitriles
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Cathepsin C