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...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Salazar, M. O., Osella, M. I., Ramallo, I. A., Furlán, Ricardo Luis Eugenio
Formato:	article artículo publishedVersion
Lenguaje:	Inglés
Publicado:	Royal Society of Chemistry 2021
Materias:	Urtica urens L. Semisynthetic Compounds Chemically Engineered Extracts Organosulfur Compounds
Acceso en línea:	http://hdl.handle.net/2133/20013 http://hdl.handle.net/2133/20013
Aporte de:	Repositorio Hipermedial de la Universidad Nacional de Rosario (UNR) de Universidad Nacional de Rosario

id	I15-R121-2133-20013
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

Nα-arylsulfonyl histamines as selective βglucosidase inhibitors

Ejemplares similares