Inhibition of the β-carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with sulphonamides

Linda J. Urbański, Andrea Angeli, Vesa P. Hytönen, Anna Di Fiore, Giuseppina De Simone, Seppo Parkkila, Claudiu T. Supuran

Research output: Contribution to journalArticleScientificpeer-review

1 Citation (Scopus)
3 Downloads (Pure)

Abstract

Sulphonamides and their isosteres are classical inhibitors of the carbonic anhydrase (CAs, EC 4.2.1.1) metalloenzymes. The protozoan pathogen Trichomonas vaginalis encodes two such enzymes belonging to the β-class, TvaCA1 and TvaCA2. Here we report the first sulphonamide inhibition study of TvaCA1, with a series of simple aromatic/heterocyclic primary sulphonamides as well as with clinically approved/investigational drugs for a range of pathologies (diuretics, antiglaucoma, antiepileptic, antiobesity, and antitumor drugs). TvaCA1 was effectively inhibited by acetazolamide and ethoxzolamide, with KIs of 391 and 283 nM, respectively, whereas many other simple or clinically used sulphonamides were micromolar inhibitors or did not efficiently inhibit the enzyme. Finding more effective TvaCA1 inhibitors may constitute an innovative approach for fighting trichomoniasis, a sexually transmitted infection, caused by T. vaginalis.

Original languageEnglish
Pages (from-to)329-334
Number of pages6
JournalJOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume36
Issue number1
Early online date28 Dec 2020
DOIs
Publication statusPublished - 2021
Publication typeA1 Journal article-refereed

Keywords

  • Carbonic anhydrase
  • inhibitor
  • sulphonamide
  • Trichomonas vaginalis
  • trichomoniasis

Publication forum classification

  • Publication forum level 1

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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