Nα-arylsulfonyl histamines as selective βglucosidase inhibitors
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Royal Society of Chemistry
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Na
-benzenesulfonylhistamine, a new semi-synthetic b-glucosidase inhibitor, was obtained by bioactivityguided isolation from a chemically engineered extract of Urtica urens L. prepared by reaction with
benzenesulfonyl chloride. In order to identify better b-glucosidase inhibitors, a new series of Na
,Ns
-diarylsulfonyl and Na
-arylsulfonyl histamine derivatives was prepared. Biological studies revealed that the
b-glucosidase inhibition was in a micromolar range for several Na
-arylsulfonyl histamine compounds of
the series, Na
-4-fluorobenzenesulfonyl histamine being the most powerful compound. Besides, this
reversible and competitive inhibitor presented a good selectivity for b-glucosidase with respect to other
target enzymes including a-glucosidase.
Para citar este articulo: RSC Adv., 2018,8, 36209-36218.
Para citar este articulo: RSC Adv., 2018,8, 36209-36218.
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