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Sulfonamides with Potent Inhibitory Action and Selectivity against the ?-Carbonic Anhydrase from Vibrio cholerae.

ABSTRACT: By using N-?-acetyl-l-lysine or GABA scaffolds and the conversion of the terminal amino group to the guanidine one, benzenesulfonamides incorporating water solubilizing moieties were synthesized. The new compounds were medium potency inhibitors of the cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isoforms I and II, and highly effective, nanomolar inhibitors of the pathogenic bacterial ?-CA from Vibrio cholerae. These sulfonamides possess good selectivity for inhibiting the bacterial over the mammalian isoforms and may be used as tools to understand the role of bacterial CAs in pathogenesis.

SUBMITTER: Ceruso M 

PROVIDER: S-EPMC4094250 | biostudies-other | 2014 Jul

REPOSITORIES: biostudies-other

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Sulfonamides with Potent Inhibitory Action and Selectivity against the α-Carbonic Anhydrase from Vibrio cholerae.

Ceruso Mariangela M   Del Prete Sonia S   Alothman Zeid Z   Capasso Clemente C   Supuran Claudiu T CT  

ACS medicinal chemistry letters 20140523 7

By using N-α-acetyl-l-lysine or GABA scaffolds and the conversion of the terminal amino group to the guanidine one, benzenesulfonamides incorporating water solubilizing moieties were synthesized. The new compounds were medium potency inhibitors of the cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isoforms I and II, and highly effective, nanomolar inhibitors of the pathogenic bacterial α-CA from Vibrio cholerae. These sulfonamides possess good selectivity for inhibiting the bacterial over the mam  ...[more]

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