Abstract
A series of mono-, di-, and tri-guanidinylated derivatives of neamine were prepared via selective guanidinylation of neamine. These molecules represent a novel scaffold as inhibitors of anthrax lethal factor zinc metalloprotease. Methods for the synthesis of these compounds are described, and structure-activity relationships among the series are analyzed. In addition, initial findings regarding the mechanism of LF inhibition for these molecules are presented.
Publication types
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Aminoglycosides / chemical synthesis*
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Aminoglycosides / pharmacology*
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Antigens, Bacterial
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Bacillus anthracis / enzymology
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Bacterial Toxins / antagonists & inhibitors*
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology
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Framycetin / chemical synthesis*
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Framycetin / pharmacology*
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Guanidine / chemistry
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Kinetics
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Metalloendopeptidases / antagonists & inhibitors
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Structure-Activity Relationship
Substances
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Aminoglycosides
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Antigens, Bacterial
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Bacterial Toxins
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Enzyme Inhibitors
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anthrax toxin
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Framycetin
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neamine
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Metalloendopeptidases
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Guanidine