• Title of article

    Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides Original Research Article

  • Author/Authors

    Anthony Bertucci، نويسنده , , Alessio Innocenti، نويسنده , , Didier Zoccola، نويسنده , , Andrea Scozzafava، نويسنده , , Sylvie Tambutté، نويسنده , , Claudiu T. Supuran، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2009
  • Pages
    5
  • From page
    5054
  • To page
    5058
  • Abstract
    The inhibition of a newly cloned coral carbonic anhydrase (CA, EC 4.2.1.1) has been investigated with a series of sulfonamides, including some clinically used derivatives (acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, benzolamide, and sulpiride, or indisulam, a compound in clinical development as antitumor drug), as well as the sulfamate antiepileptic topiramate. Some simple amino-/hydrazine-/hydroxy-substituted aromatic/heterocyclic sulfonamides have also been included in the study. All types of activity have been detected, with low potency inhibitors (KIs in the range of 163–770 nM), or with medium potency inhibitors (KIs in the range of 75.1–105 nM), whereas ethoxzolamide, several clinically used sulfonamides and heterocyclic compounds showed stronger potency, with KIs in the range of 16–48.2 nM. These inhibitors may be useful to better understand the physiological role of the Stylophora pistillata CA (STPCA) in corals and its involvement in biomineralisation in this era of global warming.
  • Keywords
    Sulfonamide , Enzyme inhibitor , Secreted enzyme , Carbonic anhydrase , Biomineralisation , Scleractinian corals
  • Journal title
    Bioorganic and Medicinal Chemistry
  • Serial Year
    2009
  • Journal title
    Bioorganic and Medicinal Chemistry
  • Record number

    1306165