Design, synthesis and biological characterization of thiazolidin-4-one derivatives as promising inhibitors of Toxoplasma gondii

Melissa D'Ascenzio, Bruna Bizzarri, Celeste De Monte, Simone Carradori, Adriana Bolasco, Daniela Secci, Daniela Rivanera, Nathan Faulhaber, Claudia Bordón, Lorraine Jones-Brando

Research output: Contribution to journalArticle

Abstract

We designed and synthesized a large number of novel thiazolidin-4-one derivatives for the evaluation of their anti-Toxoplasma gondii activity. This scaffold was functionalized at the N1-hydrazine portion with aliphatic, cycloaliphatic and (hetero)aromatic moieties. Then, a benzyl pendant was introduced at the lactamic NH of the core nucleus to evaluate the influence of this chemical modification on biological activity. The compounds were subjected to several in vitro assays to assess their anti-parasitic efficacy, cytotoxicity on fibroblasts, inhibition of tachyzoite invasion/attachment and replication after treatment. Results showed that fourteen of these thiazole-based compounds compare favorably to control compound trimethoprim in terms of parasite growth inhibition.

Original languageEnglish (US)
Pages (from-to)17-30
Number of pages14
JournalEuropean Journal of Medicinal Chemistry
Volume86
DOIs
StatePublished - Aug 19 2014

Keywords

  • Cytotoxicity
  • Host cell invasion
  • Parasite growth inhibition
  • Thiazolidin-4-one
  • Toxoplasma

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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