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IBBR publication #1875

Inhibition of the α-carbonic anhydrase from Vibrio cholerae with amides and sulfonamides incorporating imidazole moieties

De Vita D, Angeli A, Pandolfi F, Bortolami M, Costi R, Di Santo R, Suffredini E, Ceruso M, Del Prete S, Capasso C, Scipione L, Supuran CT

Journal of Enzyme Inhibition and Medicinal Chemistry 32 (1): 798-804. (2017)
doi: 10.1080/14756366.2017.1327522

We discovered novel and selective sulfonamides/amides acting as inhibitors of the alpha-carbonic anhydrase (CA, EC 4.2.1.1) from the pathogenic bacterium Vibrio cholerae (VchCA). This Gram-negative bacterium is the causative agent of cholera and colonises the upper small intestine where sodium bicarbonate is present at a high concentration. The secondary sulfonamides and amides investigated here were potent, low nanomolar VchCA inhibitors whereas their inhibition of the human cytosolic isoforms CA I and II was in the micromolar range or higher. The molecules represent an interesting lead for antibacterial agents with a possibly new mechanism of action, although their CA inhibition mechanism is unknown for the moment.

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