Journal of enzyme inhibition and medicinal chemistry · 2017
Inhibition of the α-carbonic anhydrase from Vibrio cholerae with amides and sulfonamides incorporating imidazole moieties.
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De Vita Daniela, Angeli Andrea, Pandolfi Fabiana, Bortolami Martina, Costi Roberta, Di Santo Roberto, Suffredini Elisabetta, Ceruso Mariangela, Del Prete Sonia, Capasso Clemente, Scipione Luigi, Supuran Claudiu T
Аннотация
We discovered novel and selective sulfonamides/amides acting as inhibitors of the α-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.