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Acyl Selenoureido Benzensulfonamides Show Potent Inhibitory Activity Against Carbonic Anhydrases from the Pathogenic Bacterium Vibrio Cholerae

Overview
Journal Bioorg Chem
Publisher Elsevier
Specialties Biochemistry
Chemistry
Date 2017 Sep 29
PMID 28957751
Citations 10
Authors
Affiliations
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Abstract

A series of acyl selenoureido benzensulfonamides was evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors against two Vibrio cholerae such enzymes (VchCAα over VchCAβ) belonging to the α- and β-classes, potential novel targets for anti-infective drugs development. These compounds showed strong inhibitory action against VchCAα over VchCAβ and excellent selectivity over the human (h) off-target isoforms hCA I and II. Identification of potent and possibly selective inhibitors of VchCAα and/or VchCAβ over the human counterparts may lead to pharmacological tools useful for understanding the physiological role(s) of these under-investigated proteins, possibly involved in the virulence of the bacterium and colonization of the host in bicarbonate rich regions of the gastro-intestinal tract.

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