National Research Council of Italy

Institute of Biosciences and BioResources

DISBA logo CNR logo
IBBR publication #478

Synthesis of sulfonamides with effective inhibitory action against Porphyromonas gingivalis gamma-carbonic anhydrase

Ceruso M, Del Prete S, Alothman Z, Osman SM, Scozzafava A, Capasso C, Supuran CT

Bioorganic and medicinal chemistry letters 24 (16): 4006-4010. (2014)
doi: 10.1016/j.bmcl.2014.06.024

New benzenesulfonamides incorporating GABA or N-alpha-acetyl-L-lysine scaffolds as well as guanidine functionalities as water solubilizing moieties were obtained, using 4-aminoethyl/methyl-benzenesulfonamide and metanilamide/sulfanilamide as zinc-binding motives. The new compounds were medium potency inhibitors of the widespread cytosolic human carbonic anhydrase (CA, EC 4.2.1.1) isoforms I and II and more effective inhibitors (K(I)s low nanomolar range) of the bacterial gamma-CA from the oral pathogen Porphyromonas gingivalis. These sulfonamides may be useful tools for understanding the physiological role of bacterial CAs in pathogenesis of some infectious disease. (C) 2014 Elsevier Ltd. All rights reserved.

IBBR Authors:
Actions
Select by Year
Select by Type
Select by Author
*
*
*
*
Istituto di Bioscienze e Biorisorse (IBBR/CNR)
Via G. Amendola 165/A, I-70126 Bari (Italy)
Copyright © 2012-2024. All Rights Reserved.