Author/Authors :
Pingzhu Zhang، نويسنده , , Chao Wei، نويسنده , , Enkai Wang، نويسنده , , Wei Wang، نويسنده , , Ming Liu، نويسنده , , Qingmei Yin، نويسنده , , Hua Chen، نويسنده , , Kerang Wang، نويسنده , , Xiaoliu Li، نويسنده , , Jinchao Zhang، نويسنده ,
Abstract :
A series of novel isoxazoline linked pseudodisaccharide derivatives were regiospecifically synthesized by 1,3-dipolar cycloaddition of α-allyl-C-glycopyranosides and sugar-derived nitrile oxides with good yields. The structures of the compounds were characterized by NMR spectroscopy and MS spectrometry and confirmed by the X-ray crystallographic analysis of compound ((5S)-3-(2,3-O-isopropylidene-5-deoxy-d-lyxofuranose-4-yl)isoxazoline-5-yl) methyl α- C-d-galactopyranoside. Their biological activities against glycosidases (α-amylase, α-glucosidase, and β-glucosidase) and HIV-RT, and antitumor activity were preliminarily evaluated. Some of them exhibited potent inhibitory activity to HIV-RT.
Keywords :
3-dipolar cycloaddition , HIV-RT inhibition , Pseudodisaccharide , Nitrile oxide , Isoxazoline , 1