Synthesis of some natural sulphonamide derivatives as carbonic anhydrase inhibitors

Taner Gokcen*, Melike Al, Meryem Topal, Ilhami Gulcin, Turan Ozturk, Ahmet C. Goren

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

23 Citations (Scopus)

Abstract

Carbonic anhydrase inhibitors are both in clinical use as antiglaucoma, diuretics, antiepileptics and management of altitude sickness, and under investigation as anticancer, anticonvulsant and antiobesity agents. Sulphonamides have been known for decades as carbonic anhydrase inhibitors and are in clinical use. Sulphonamide derivatives of p-hydroxybenzoic acid and 3,4,5-trihydroxybenzoic acid (gallic acid) were synthesized and their inhibition values over hCA I and hCA II isozymes, purified from human erythrocyte cells by Sepharose-4B-L-tyrosine-sulphanilamide, were determined. Compounds synthesized showed efficient carbonic anhydrase inhibition activity at low nM levels.

Original languageEnglish
Pages (from-to)15-23
Number of pages9
JournalOrganic Communications
Volume10
Issue number1
DOIs
Publication statusPublished - 2017

Bibliographical note

Publisher Copyright:
© 2017 ACG Publications.

Keywords

  • 3,4,5-trihydroxybenzoic acid (gallic acid)
  • Carbonic anhydrase inhibitor
  • p-hydroxybenzoic acid
  • Sulphonamides

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