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Arylsulfonyl histamine derivatives as powerful and selective α-glucosidase inhibitors

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Abstract

A series of simple N-arylbenzenesulfonyl histamine derivatives were prepared and screened against α-glucosidase. Inhibition was in the micromolar range for several Nα,Nτ-di-arylsulfonyl compounds, with Nα,Nτ-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 acarbose with half of its dose.

Graphical abstract: Arylsulfonyl histamine derivatives as powerful and selective α-glucosidase inhibitors

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Article information


Submitted
29 Nov 2019
Accepted
17 Feb 2020
First published
12 Mar 2020

RSC Med. Chem., 2020, Advance Article
Article type
Research Article

Arylsulfonyl histamine derivatives as powerful and selective α-glucosidase inhibitors

M. I. Osella, M. O. Salazar, M. D. Gamarra, D. M. Moreno, F. Lambertucci, D. E. Frances and R. L. E. Furlan, RSC Med. Chem., 2020, Advance Article , DOI: 10.1039/C9MD00559E

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