• Marta Ferraroni
  • Laura Lucarini
  • Emanuela Masini
  • Mikhail Korsakov
  • Andrea Scozzafava
  • Claudiu T. Supuran
  • Mikhail Krasavin

Two lead 1,3-oxazole-based carbonic anhydrase inhibitors (CAIs) earlier identified as selective, picomolar inhibitors of hCA II (a cytosolic target for treatment of glaucoma) have been investigated further. Firstly, they were found to be conveniently synthesized on multigram scale, which enables further development. These compounds were found to be comparable in efficacy to dorzolamide eye drops when applied in the eye drop form as well. Finally, the reasons for unusually high potency of these compounds became understood from their high-resolution X-ray crystallography structures. These data significantly expand our understanding of heterocycle-based primary sulfonamides, many of which have recently emerged from our labs - particularly, from the corneal permeability standpoint.

Original languageEnglish
Pages (from-to)4560-4565
Number of pages6
JournalBioorganic and Medicinal Chemistry
Volume25
Issue number17
DOIs
StatePublished - 1 Sep 2017

    Research areas

  • Carbonic anhydrase inhibitors, Isoform selectivity, Multigram synthesis, Ocular hypertension, Picomolar inhibition, Primary sulfonamide, X-ray crystallography

    Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

ID: 34636078