Nα-arylsulfonyl histamines as selective βglucosidase inhibitors
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...
Guardado en:
| Autores principales: | , , , |
|---|---|
| Formato: | article artículo publishedVersion |
| Lenguaje: | Inglés |
| Publicado: |
Royal Society of Chemistry
2021
|
| Materias: | |
| Acceso en línea: | http://hdl.handle.net/2133/20013 http://hdl.handle.net/2133/20013 |
| Aporte de: |
| Sumario: | 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. |
|---|