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...
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Autores principales: | , , , |
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Formato: | article artículo publishedVersion |
Lenguaje: | Inglés |
Publicado: |
Royal Society of Chemistry
2021
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Materias: | |
Acceso en línea: | http://hdl.handle.net/2133/20013 http://hdl.handle.net/2133/20013 |
Aporte de: |
id |
I15-R121-2133-20013 |
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record_format |
dspace |
institution |
Universidad Nacional de Rosario |
institution_str |
I-15 |
repository_str |
R-121 |
collection |
Repositorio Hipermedial de la Universidad Nacional de Rosario (UNR) |
language |
Inglés |
orig_language_str_mv |
eng |
topic |
Urtica urens L. Semisynthetic Compounds Chemically Engineered Extracts Organosulfur Compounds |
spellingShingle |
Urtica urens L. Semisynthetic Compounds Chemically Engineered Extracts Organosulfur Compounds Salazar, M. O. Osella, M. I. Ramallo, I. A. Furlán, Ricardo Luis Eugenio Nα-arylsulfonyl histamines as selective βglucosidase inhibitors |
topic_facet |
Urtica urens L. Semisynthetic Compounds Chemically Engineered Extracts Organosulfur Compounds |
description |
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. |
format |
article artículo publishedVersion |
author |
Salazar, M. O. Osella, M. I. Ramallo, I. A. Furlán, Ricardo Luis Eugenio |
author_facet |
Salazar, M. O. Osella, M. I. Ramallo, I. A. Furlán, Ricardo Luis Eugenio |
author_sort |
Salazar, M. O. |
title |
Nα-arylsulfonyl histamines as selective βglucosidase inhibitors |
title_short |
Nα-arylsulfonyl histamines as selective βglucosidase inhibitors |
title_full |
Nα-arylsulfonyl histamines as selective βglucosidase inhibitors |
title_fullStr |
Nα-arylsulfonyl histamines as selective βglucosidase inhibitors |
title_full_unstemmed |
Nα-arylsulfonyl histamines as selective βglucosidase inhibitors |
title_sort |
nα-arylsulfonyl histamines as selective βglucosidase inhibitors |
publisher |
Royal Society of Chemistry |
publishDate |
2021 |
url |
http://hdl.handle.net/2133/20013 http://hdl.handle.net/2133/20013 |
work_keys_str_mv |
AT salazarmo naarylsulfonylhistaminesasselectivebglucosidaseinhibitors AT osellami naarylsulfonylhistaminesasselectivebglucosidaseinhibitors AT ramalloia naarylsulfonylhistaminesasselectivebglucosidaseinhibitors AT furlanricardoluiseugenio naarylsulfonylhistaminesasselectivebglucosidaseinhibitors |
bdutipo_str |
Repositorios |
_version_ |
1764820411248279556 |