title: Sulfonamides with Potent Inhibitory Action and Selectivity against the α-Carbonic Anhydrase from Vibrio cholerae.
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.
authors: Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Università degli Studi di Firenze , Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino, Firenze, Italy.
authors: Mariangela
authors: M
authors: Ceruso
authors: Istituto di Bioscienze e Biorisorse, CNR , Via Pietro Castellino 111, 80131 Napoli, Italy.
authors: Sonia
authors: S
authors: Del Prete
authors: Department of Chemistry, College of Science, King Saud University , Riyadh 11451, Saudi Arabia.
authors: Zeid
authors: Z
authors: Alothman
authors: Istituto di Bioscienze e Biorisorse, CNR , Via Pietro Castellino 111, 80131 Napoli, Italy.
authors: Clemente
authors: C
authors: Capasso
authors: Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Università degli Studi di Firenze , Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino, Firenze, Italy ; Department of Chemistry, College of Science, King Saud University , Riyadh 11451, Saudi Arabia ; Neurofarba Department, Section of Pharmaceutical and Nutriceutical Sciences, Università degli Studi di Firenze , Via U. Schiff 6, 50019 Sesto Fiorentino, Florence, Italy.
authors: Claudiu T
authors: CT
authors: Supuran
keywords: Carbonic anhydrase; Vibrio cholerae; amino acid; enzyme inhibitor; sulfonamide