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IBBR publication #1830

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

Angeli A, Abbas G, Del Prete S, Carta F, Capasso C, Supuran CT

Bioorganic Chemistry 75: 170-172. (2017)
doi: 10.1016/j.bioorg.2017.09.016

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? over VchCA?) belonging to the ?- and ?-classes, potential novel targets for anti-infective drugs development. These compounds showed strong inhibitory action against VchCA? over VchCA? and excellent selectivity over the human (h) off-target isoforms hCA I and II. Identification of potent and possibly selective inhibitors of VchCA? and/or VchCA? 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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