Journal of Enzyme Inhibition and Medicinal Chemistry (Jan 2020)

Toxicity evaluation of sulfamides and coumarins that efficiently inhibit human carbonic anhydrases

  • Ashok Aspatwar,
  • Emanuela Berrino,
  • Silvia Bua,
  • Fabrizio Carta,
  • Clemente Capasso,
  • Seppo Parkkila,
  • Claudiu T. Supuran

DOI
https://doi.org/10.1080/14756366.2020.1822829
Journal volume & issue
Vol. 35, no. 1
pp. 1765 – 1772

Abstract

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Here, we report a toxicity study, conducted on zebrafish larvae, of a series of coumarin and sulfamide compounds that were previously reported as inhibitors of human (h) metalloenzymes, carbonic anhydrases (CAs, EC 4.2.1.1). Due to the high relevance of hCA inhibitors as theragnostic agents, it is of pivotal importance to address safety issues that may arise from the initial in vivo toxicological assessment using zebrafish, a relevant model for biomedical research. None of the reported compounds showed adverse phenotypic effects or tissue damage on developing zebrafish larvae after 5 days of exposure. Our study suggests that the coumarin and sulfamide derivatives considered here are safe and suitable for further development and testing.

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