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Characterization of antimicrobial, antioxidant, and leishmanicidal activities of Schiff base derivatives of 4-aminoantipyrine

  • Rommy Teran
  • , Rommel Guevara
  • , Jessica Mora
  • , Lizeth Dobronski
  • , Olalla Barreiro-Costa
  • , Timo Beske
  • , Jorge Pérez-Barrera
  • , Ramiro Araya-Maturana
  • , Patricio Rojas-Silva
  • , Ana Poveda*
  • , Jorge Heredia-Moya
  • *Corresponding author for this work
  • Universidad Central del Ecuador
  • Universidad de las Americas - Ecuador
  • Universidad Tecnológica Equinoccial
  • Universidad de Talca

Research output: Contribution to journalArticlepeer-review

76 Scopus citations

Abstract

Our main interest is the characterization of compounds to support the development of alternatives to currently marketed drugs that are losing effectiveness due to the development of resistance. Schiff bases are promising biologically interesting compounds having a wide range of pharmaceutical properties, including anti-inflammatory, antipyretic, and antimicrobial activities, among others. In this work, we have synthesized 12 Schiff base derivatives of 4-aminoantipyrine. In vitro antimicrobial, antioxidant, and cytotoxicity properties are analyzed, as well as in silico predictive adsorption, distribution, metabolism, and excretion (ADME) and bioactivity scores. Results identify two potential Schiff bases: one effective against E. faecalis and the other with antioxidant activity. Both have reasonable ADME scores and provides a scaffold for developing more effective compounds in the future. Initial studies are usually limited to laboratory in vitro approaches, and following these initial studies, much research is needed before a drug can reach the clinic. Nevertheless, these laboratory approaches are mandatory and constitute a first filter to discriminate among potential drug candidates and chemical compounds that should be discarded.

Original languageEnglish
Article number2696
JournalMolecules
Volume24
Issue number15
DOIs
StatePublished - 24 Jul 2019
Externally publishedYes

Keywords

  • Antimicrobial activity
  • Cytotoxicity
  • Leishmania
  • Schiff base synthesis

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