Benzimidazo[1,2-c][1,2,3]thiadiazole-7-sulfonamides as inhibitors of carbonic anhydrase

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3335-8. doi: 10.1016/j.bmcl.2007.03.100. Epub 2007 Apr 5.

Abstract

A series of benzimidazo[1,2-c][1,2,3]thiadiazole-7-sulfonamides were synthesized and their binding to two carbonic anhydrase isozymes measured by isothermal titration calorimetry (ITC). Human carbonic anhydrase I (hCAI) and bovine carbonic anhydrase II (bCAII) bound the inhibitors with observed association constants in the range from 1.1 x 10(6) to 2.6 x 10(7) M(-1).

MeSH terms

  • Animals
  • Benzimidazoles / chemical synthesis
  • Benzimidazoles / pharmacology*
  • Binding Sites
  • Calorimetry / methods
  • Carbonic Anhydrase I / antagonists & inhibitors*
  • Carbonic Anhydrase II / antagonists & inhibitors*
  • Carbonic Anhydrase Inhibitors / chemical synthesis
  • Carbonic Anhydrase Inhibitors / pharmacology*
  • Cattle
  • Humans
  • Structure-Activity Relationship
  • Sulfonamides / chemical synthesis
  • Sulfonamides / pharmacology*
  • Titrimetry / methods

Substances

  • Benzimidazoles
  • Carbonic Anhydrase Inhibitors
  • Sulfonamides
  • Carbonic Anhydrase I
  • Carbonic Anhydrase II