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

• Main Authors: Daniela De Vita (Author), Andrea Angeli (Author), Fabiana Pandolfi (Author), Martina Bortolami (Author), Roberta Costi (Author), Roberto Di Santo (Author), Elisabetta Suffredini (Author), Mariangela Ceruso (Author), Sonia Del Prete (Author), Clemente Capasso (Author), Luigi Scipione (Author), Claudiu T. Supuran (Author)
• Format: Book
• Published: Taylor & Francis Group, 2017-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Summary

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.

Item Description

1475-6366
1475-6374
10.1080/14756366.2017.1327522