4.7 Article

Acyl selenoureido benzensulfonamides show potent inhibitory activity against carbonic anhydrases from the pathogenic bacterium Vibrio cholerae

Journal

BIOORGANIC CHEMISTRY
Volume 75, Issue -, Pages 170-172

Publisher

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2017.09.016

Keywords

Carbonic anhydrase; Inhibitors; Metalloenzymes; Selenium; Acylseleno-ureido; Vibrio cholerae

Ask authors/readers for more resources

A series of acyl selenoureido benzensulfonamides was evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors against two Vibrio cholerae such enzymes (VchCA alpha over VchCA beta) belonging to the alpha- and beta-classes, potential novel targets for anti-infective drugs development. These compounds showed strong inhibitory action against VchCA alpha over VchCA beta and excellent selectivity over the human (h) off-target isoforms hCA I and II. Identification of potent and possibly selective inhibitors of VchCA alpha and/or VchCA beta 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. (C) 2017 Elsevier Inc. All rights reserved.

Authors

I am an author on this paper
Click your name to claim this paper and add it to your profile.

Reviews

Primary Rating

4.7
Not enough ratings

Secondary Ratings

Novelty
-
Significance
-
Scientific rigor
-
Rate this paper

Recommended

No Data Available
No Data Available