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 mammalian isoforms and may be used as tools to understand the role of bacterial CAs in pathogenesis.
Sulfonamides with potent inhibitory action and selectivity against the α-carbonic anhydrase from Vibrio cholerae / Ceruso, Mariangela; Del Prete, Sonia; Alothman, Zeid; Capasso, Clemente; Supuran, Claudiu T.. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - STAMPA. - 5:(2014), pp. 826-830. [10.1021/ml500192a]
Sulfonamides with potent inhibitory action and selectivity against the α-carbonic anhydrase from Vibrio cholerae
CERUSO, MARIANGELA;DEL PRETE, SONIA;SUPURAN, CLAUDIU TRANDAFIR
2014
Abstract
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 mammalian isoforms and may be used as tools to understand the role of bacterial CAs in pathogenesis.
I documenti in FLORE sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
