Abstract
A straightforward strategy for the synthesis of triazole-containing MraY inhibitors has been developed. It involves the sequential introduction of a terminal alkyne at the 5' position of an uridine derivative and O-glycosylation with a protected aminoribose leading to an elaborated alkyne scaffold. An efficient Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) allowed the introduction of chemical diversity toward a small library of inhibitors.
MeSH terms
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Alkynes / chemistry
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Anti-Bacterial Agents / chemical synthesis*
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Anti-Bacterial Agents / chemistry
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Azides / chemistry
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Bacterial Proteins / antagonists & inhibitors*
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Bacterial Proteins / chemistry*
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Catalysis
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Copper / chemistry*
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Cycloaddition Reaction
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Drug Resistance, Bacterial
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Glycosylation
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Transferases (Other Substituted Phosphate Groups)
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Transferases / antagonists & inhibitors*
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Transferases / chemistry*
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Triazoles / chemical synthesis*
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Triazoles / chemistry
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Uridine / chemical synthesis*
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Uridine / chemistry
Substances
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Alkynes
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Anti-Bacterial Agents
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Azides
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Bacterial Proteins
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Enzyme Inhibitors
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Triazoles
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Copper
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Transferases
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Transferases (Other Substituted Phosphate Groups)
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mraY protein, Bacteria
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Uridine