Issue 63, 2018

Nα-arylsulfonyl histamines as selective β-glucosidase inhibitors

Abstract

N α -benzenesulfonylhistamine, a new semi-synthetic β-glucosidase inhibitor, was obtained by bioactivity-guided isolation from a chemically engineered extract of Urtica urens L. prepared by reaction with benzenesulfonyl chloride. In order to identify better β-glucosidase inhibitors, a new series of Nα,Nτ-di-arylsulfonyl and Nα-arylsulfonyl histamine derivatives was prepared. Biological studies revealed that the β-glucosidase inhibition was in a micromolar range for several Nα-arylsulfonyl histamine compounds of the series, Nα-4-fluorobenzenesulfonyl histamine being the most powerful compound. Besides, this reversible and competitive inhibitor presented a good selectivity for β-glucosidase with respect to other target enzymes including α-glucosidase.

Graphical abstract: Nα-arylsulfonyl histamines as selective β-glucosidase inhibitors

Supplementary files

Article information

Article type
Paper
Submitted
07 Aug 2018
Accepted
19 Oct 2018
First published
24 Oct 2018
This article is Open Access
Creative Commons BY license

RSC Adv., 2018,8, 36209-36218

N α -arylsulfonyl histamines as selective β-glucosidase inhibitors

M. O. Salazar, M. I. Osella, I. A. Ramallo and R. L. E. Furlan, RSC Adv., 2018, 8, 36209 DOI: 10.1039/C8RA06625F

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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