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

Autor: Daniela De Vita, Andrea Angeli, Fabiana Pandolfi, Martina Bortolami, Roberta Costi, Roberto Di Santo, Elisabetta Suffredini, Mariangela Ceruso, Sonia Del Prete, Clemente Capasso, Luigi Scipione, Claudiu T. Supuran
Jazyk: angličtina
Rok vydání: 2017
Předmět:
Zdroj: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 32, Iss 1, Pp 798-804 (2017)
Druh dokumentu: article
ISSN: 1475-6366
1475-6374
14756366
DOI: 10.1080/14756366.2017.1327522
Popis: 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.
Databáze: Directory of Open Access Journals
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