Evaluation of Thio- and Seleno-Acetamides Bearing Benzenesulfonamide as Inhibitor of Carbonic Anhydrases from Different Pathogenic Bacteria

评价含苯磺酰胺的硫代乙酰胺和硒代乙酰胺作为不同致病菌碳酸酐酶抑制剂的效果

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作者:Andrea Angeli, Mariana Pinteala, Stelian S Maier, Bogdan C Simionescu, Andrea Milaneschi, Ghulam Abbas, Sonia Del Prete, Clemente Capasso, Antonella Capperucci, Damiano Tanini, Fabrizio Carta, Claudiu T Supuran

Abstract

A series of 2-thio- and 2-seleno-acetamides bearing the benzenesulfonamide moiety were evaluated as Carbonic Anhydrase (CA, EC 4.2.1.1) inhibitors against different pathogenic bacteria such as the Vibrio cholerae (VchCA-α and VchCA-β), Burkholderia pseudomallei (BpsCA-β and BpsCA-γ), Mycobacterium tuberculosis (Rv3723-β) and the Salmonella enterica serovar Typhimurium (StCA2-β). The molecules represent interesting leads worth developing as innovative antibacterial agents since they possess new mechanism of action and isoform selectivity preferentially against the bacterial expressed CAs. The identification of potent and selective inhibitors of bacterial CAs may lead to tools also useful for deciphering the physiological role(s) of such proteins.

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