Author/Authors :
Robert ?ysek، نويسنده , , Catherine Schütz، نويسنده , , Sylvain Favre، نويسنده , , Anthony C. O’Sullivan، نويسنده , , Christian Pillonel، نويسنده , , Thomas Krülle، نويسنده , , Pierre M.J. Jung، نويسنده , , Imma Clotet-Codina، نويسنده , , José A. Esté، نويسنده , , Jean-Claude Hausmann and Pierre Vogel، نويسنده ,
Abstract :
A solid-phase synthesis of new N-substituted valienamines has been developed and new synthesis of (±)-conduramine F-1, (−)-conduramine F-1, and (+)-ent-conduramine F-1 is presented, together with the preparation of N-benzylated conduramines F-1. N-Benzylation of both valienamine and (+)-ent-conduramine F-1 improves their inhibitory activity toward α-glucosidases significantly. The additional hydroxymethyl group makes valienamine derivatives more active than their (+)-ent-conduramine F-1 analogues.
Keywords :
‘Naked sugars’ , Imines , Cytotoxicity , Conduramine F-1 (aminoconduritol) , Solid-phase synthesis , ?-Glucosidase inhibitors
