Glycogen phosphorylase inhibitors are considered as potential antidiabetic agents. 3-(β-d-Glucopyranosyl)-5-substituted-1,2,4-triazoles were prepared by acylation of O-perbenzoylated N (1)-tosyl-C-β-d-glucopyranosyl formamidrazone and subsequent removal of the protecting groups. The best inhibitor was 3-(β-d-glucopyranosyl)-5-(2-naphthyl)-1,2,4-triazole (K i = 0.41 μM against rabbit muscle glycogen phosphorylase b).
Keywords: 1,2,4-Triazole; C-glucopyranosyl derivative; bioisoster; glycogen phosphorylase; inhibitor.