Arylsulfonyl histamine derivatives as powerful and selective α-glucosidase inhibitors.

A series of simple -arylbenzenesulfonyl histamine derivatives were prepared and screened against α-glucosidase. Inhibition was in the micromolar range for several , -di-arylsulfonyl compounds, with , -di-4-trifluorobenzenesulfonyl histamine () being the best inhibitor. Compound is a reversible and competitive α-glucosidase inhibitor, and presented good selectivity with respect to other target enzymes, including β-glucosidase and α-amylase, and interesting predicted physicochemical properties. Docking studies have been run to postulate ligand-enzyme interactions to account for the experimental results. , compound produced a similar hypoglycemic effect to acarbose with half of its dose.