Nᵅ-arylsulfonyl histamines as selective β-glucosidase inhibitors
2018
Salazar, M. O. | Osella, M. I. | Ramallo, I. A. | Furlan, R. L. E.
Nᵅ-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 Nᵅ,Nτ-di-arylsulfonyl and Nᵅ-arylsulfonyl histamine derivatives was prepared. Biological studies revealed that the β-glucosidase inhibition was in a micromolar range for several Nᵅ-arylsulfonyl histamine compounds of the series, Nᵅ-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.
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