Abstract
By screening a library of metalloenzyme inhibitors, the N-formyl-hydroxylamine derivative BB-3497 was identified as a potent inhibitor of Escherichia coli peptide deformylase with antibacterial activity both in vitro and in vivo. The homochiral synthesis of BB-3497, involving a novel asymmetric Michael addition reaction is described.
MeSH terms
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Amidohydrolases*
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Aminopeptidases / antagonists & inhibitors*
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology
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Crystallography, X-Ray
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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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Hydroxamic Acids / chemical synthesis*
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Hydroxamic Acids / chemistry
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Hydroxamic Acids / pharmacology
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Molecular Conformation
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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BB3497
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Enzyme Inhibitors
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Hydroxamic Acids
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Aminopeptidases
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Amidohydrolases
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peptide deformylase
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actinonin