摘要
Triazolyl phenylalanine and tyrosine-aryl C-glycoside hybrids were readily synthesized via microwave-assisted Cu（I）-catalyzed azide-alkyne 1,3-dipolar cycloaddition in high yields. Successive enzymatic assay identified the synthesized glycoconjugates as novel PTPlB inhibitors with low micromole-ranged inhibitory activity and at least several-fold selectivity over other homologous PTPs tested found crucial toward PTP1 B inhibition. In addition, the benzyl groups on glucosyl moiety were
Triazolyl phenylalanine and tyrosine-aryl C-glycoside hybrids were readily synthesized via microwave-assisted Cu（I）-catalyzed azide-alkyne 1,3-dipolar cycloaddition in high yields. Successive enzymatic assay identified the synthesized glycoconjugates as novel PTPlB inhibitors with low micromole-ranged inhibitory activity and at least several-fold selectivity over other homologous PTPs tested found crucial toward PTP1 B inhibition. In addition, the benzyl groups on glucosyl moiety were
