Inhibition of the ?-carbonic anhydrase from Vibrio cholerae with amides and sulfonamides incorporating imidazole moieties
01 Pubblicazione su rivista
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.
ISSN: 1475-6366
We discovered novel and selective sulfonamides/amides acting as inhibitors of the a-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.