Author/Authors :
Best، نويسنده , , Daniel and Jenkinson، نويسنده , , Sarah F. and Saville، نويسنده , , A. Waldo and Alonzi، نويسنده , , Dominic S. and Wormald، نويسنده , , Mark R. and Butters، نويسنده , , Terry D. and Norez، نويسنده , , Caroline and Becq، نويسنده , , Frederic and Blériot، نويسنده , , Yves and Adachi، نويسنده , , Isao and Kato، نويسنده , , Atsushi and Fleet، نويسنده , , George W.J.، نويسنده ,
Abstract :
Acetonides are the only protecting groups used in the syntheses of isoDAB from d-ribose and of isoLAB from d-tagatose. isoDAB is a potent and highly specific competitive α-glucosidase inhibitor (for rice α-glucosidase, Ki = 4 μM for isoDAB compared to Ki 14 μM for DAB). isoDAB is not an—whereas DAB is a potent—inhibitor of glycogen phosphorylase. This is the first example of any potent inhibition of glycosidases by a carbon-branched iminosugar pyrrolidine. Although isoLAB shows no inhibition of any glycosidase, preliminary experiments suggest that isoLAB partially rescues the defective F508del-CFTR function and so may have a role in the study of cystic fibrosis.
