Journal
BIOORGANIC CHEMISTRY
Volume 75, Issue -, Pages 170-172Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2017.09.016
Keywords
Carbonic anhydrase; Inhibitors; Metalloenzymes; Selenium; Acylseleno-ureido; Vibrio cholerae
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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.
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