In vitro inhibition of cytosolic carbonic anhydrases I and II by some new dihydroxycoumarin compounds

J Enzyme Inhib Med Chem. 2008 Feb;23(1):32-6. doi: 10.1080/14756360701404100.

Abstract

A new series of 6, 7-dihydroxy-3-(methylphenyl) chromenones, including three new derivatives, i.e. 6,7-dihydroxy-3-(2-methylphenyl)-2H-chromen-2-one (OPC); 6,7-dihydroxy-3-(3-methylphenyl)-2H-chromen-2-one (MPC); 6,7-dihydroxy-3-(4-methylphenyl)-2H-chromen-2-one (PPC) and one previously described, namely 6,7-dihydroxy-3-phenyl-2H-chromen-2-one (DPC), were synthesized. These compounds were investigated as inhibitors of human carbonic anhydrase I (hCA-I) and human carbonic anhydrase II (hCA-II) which had been purified from human erythrocytes on an affinity gel comprised of L-tyrosine-sulfonamide-Sepharose 4B.

MeSH terms

  • Carbonic Anhydrase I / antagonists & inhibitors*
  • Carbonic Anhydrase II / antagonists & inhibitors*
  • Coumarins / pharmacology*
  • Cytosol / enzymology
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Hydroxylation
  • Kinetics

Substances

  • Coumarins
  • Enzyme Inhibitors
  • Carbonic Anhydrase I
  • Carbonic Anhydrase II