Based on “Click chemistry”, A series of glycosyltriazole salicylic acid derivatives using glycosyl azide and alkynyl-substituted salicylaldehyde as starting material were synthesized via copper-mediated 1,3-dipolar cycloaddition reactions, oxidation and hydrolysis reaction. The structure was characterized by 1H-NMR, IR, ESI-MS and elemental analysis. These compounds were evaluated for their PTP1B inhibitory activity. The results demonstrated that all compounds presented potent inhibitory activities against PTP1B, among which compounds 4a exhibited most potent with IC50 value of 54.52?0.79μM.