Conformationally locked thiosugars as potent α-mannosidase inhibitors: Synthesis, biochemical and docking studies

Abstract

A series of thiosugar derivatives (thiolevomannosans) derived from mannose were synthesized and their inhibitory activity was tested against α-mannosidase (jack bean). These inhibitors were found to be more potent than the well-known inhibitors like kifunensine and deoxymannojirimycin based on docking and biochemical studies. The sulfone derivative 10 was shown to be the best inhibitor of α-mannosidase with the K i value of 350 nM.