We discovered novel and selective sulfonamides/amides acting as inhibitors of the α-carbonic anhydrase (CA, EC 126.96.36.199) 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.
|Number of pages||7|
|Journal||Journal of Enzyme Inhibition and Medicinal Chemistry|
|Publication status||Published - Jan 1 2017|
- Carbonic anhydrase
- Vibrio cholerae
ASJC Scopus subject areas
- Drug Discovery