Synthesis of sugar-amino acid-nucleosides as potential glycosyltransferase inhibitors

Potential galactosyltransferase inhibitors were synthesized by replacing the diphosphate moiety in sugar donor with a basic amino acid. Analogues containing tryptophan and histidine showed moderate inhibition against mycobacterial GlfT2, which we suggest may arise by mimicking the interaction between the diphosphate metal ion complex with the carboxylate residues present in the active site of the enzyme.