Synthesis and carbonic anhydrase inhibitory properties of 1,3-dicarbonyl derivatives of methylaminobenzene-sulfonamide

J Enzyme Inhib Med Chem. 2014 Feb;29(1):132-6. doi: 10.3109/14756366.2012.757603. Epub 2013 Jan 28.


Abstract 1,3-Dicarbonyl derivatives of methylaminobenzene-sulfonamide were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I and hCA II were evaluated. hCA I and hCA II from human erythrocytes were purified by a simple one-step procedure by using Sepharose 4B-L-tyrosine-sulfanilamide affinity column. Our results show that the synthesized compounds inhibited the activity of carbonic anhydrase (CA) I and CA II. Among them, 2b and 2e were found to be the most active (IC50=2.12 and 2.52 µM) for hCA I and hCA II, respectively.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Carbonic Anhydrase Inhibitors / chemical synthesis*
  • Carbonic Anhydrase Inhibitors / pharmacology*
  • Chromatography, Affinity
  • Erythrocytes / enzymology
  • Humans
  • Sulfonamides / chemical synthesis*
  • Sulfonamides / pharmacology*


  • Carbonic Anhydrase Inhibitors
  • Sulfonamides