Abstract
The appearance multi-drug resistant Mycobacterium tuberculosis (MTB) throughout the world has prompted a search for new, safer and more active agents against tuberculosis. Based on studies of the biosynthesis of mycobacterial cell wall polysaccharides, octyl 5-O-(alpha-D-arabinofuranosyl)-alpha-D-arabinofuranoside analogues were synthesized and evaluated as inhibitors for M. tuberculosis and Mycobacterium avium. A cell free assay system has been used for the evaluation of these disaccharides as substrates for mycobacterial arabinosyltransferase activity.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Antitubercular Agents / chemistry*
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Antitubercular Agents / metabolism*
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Antitubercular Agents / pharmacology
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Carbohydrate Conformation
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Disaccharides / chemistry*
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Disaccharides / metabolism*
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Disaccharides / pharmacology
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Drug Evaluation, Preclinical
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Inhibitory Concentration 50
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Mycobacterium avium / drug effects
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Mycobacterium avium / enzymology
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Mycobacterium tuberculosis / drug effects
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Mycobacterium tuberculosis / enzymology*
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Pentosyltransferases / antagonists & inhibitors
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Pentosyltransferases / metabolism*
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Structure-Activity Relationship
Substances
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Antitubercular Agents
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Disaccharides
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Pentosyltransferases
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arabinosyltransferase