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

Research output: Contribution to journalArticleScientificpeer-review

1 Citation (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)1765-1772
Number of pages8
JournalJOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume35
Issue number1
DOIs
Publication statusPublished - 2020
Publication typeA1 Journal article-refereed

Keywords

  • Carbonic anhydrases
  • inhibitors
  • toxicity screening
  • zebrafish

Publication forum classification

  • Publication forum level 1

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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