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

ABSTRACT: A series of simple N-arylbenzenesulfonyl histamine derivatives were prepared and screened against α-glucosidase. Inhibition was in the micromolar range for several N ^α,N ^τ-di-arylsulfonyl compounds, with N ^α,N ^τ-di-4-trifluorobenzenesulfonyl histamine (IId) being the best inhibitor. Compound IId 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. In vivo, compound IId produced a similar hypoglycemic effect to ac

SUBMITTER: Osella MI 

PROVIDER: S-EPMC7489258 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature