Abstract
Efforts to modify the central proline portion of lead compound 4 lead to the discovery of novel prolylcarboxypeptidase (PrCP) inhibitors. Especially, replacement with alanine afforded compound 19 displaying more potent human and mouse PrCP inhibitory activity than 4 and an overall comparable profile.
Copyright © 2011. Published by Elsevier Ltd.
MeSH terms
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Alanine / chemistry*
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Alanine / pharmacology
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Animals
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Carboxypeptidases / antagonists & inhibitors*
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Drug Discovery*
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Enzyme Activation / drug effects
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Humans
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Inhibitory Concentration 50
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Mice
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Molecular Structure
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Carboxypeptidases
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lysosomal Pro-X carboxypeptidase
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Alanine