Abstract
Guided by the inhibitory activities of indole-containing natural products against isocitrate lyase (ICL) from Candida albicans and sortase A (SrtA) from Staphylococcus aureus, a series of compounds structurally analogous to natural products were synthesized. Eight SrtA inhibitors and an ICL inhibitor having higher activities than the natural products were discovered by screening the enzyme inhibitory activities of synthesized compounds. Among the SrtA inhibitors discovered, six exhibited higher activities than p-hydroxymercuribenzoic acid, which suggests that these compounds have great potential as alternative antibacterial agents.
Copyright © 2010 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aminoacyltransferases / antagonists & inhibitors*
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Anti-Bacterial Agents / chemistry*
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Anti-Bacterial Agents / pharmacology
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Bacterial Proteins / antagonists & inhibitors*
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Biological Products / chemistry*
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Candida albicans / enzymology
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Cysteine Endopeptidases
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Drug Evaluation, Preclinical / methods
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology
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Indoles / chemical synthesis
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Indoles / chemistry*
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Indoles / pharmacology
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Isocitrate Lyase / antagonists & inhibitors*
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Staphylococcus aureus / enzymology
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Bacterial Proteins
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Biological Products
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Enzyme Inhibitors
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Indoles
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Aminoacyltransferases
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sortase A
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Cysteine Endopeptidases
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Isocitrate Lyase