Design, synthesis and biological evaluation of small molecules as potent glucosidase inhibitors

Herein we have reported design, synthesis and in vitro biological evaluation of a library of bicyclic lactams that led to the discovery of compounds 6 and 7 as a novel class of a-glucosidase inhibitors. They inhibited alpha-glucosidase (yeast origin) in a mixed type of inhibition with an IC50 of similar to 150 nM. Molecular docking studies further substantiated screening results. Interestingly phenotypic screening of this library against the human malaria parasite revealed 7 as a potent antiplasmodial agent. (C) 2015 Elsevier Masson SAS. All rights reserved.