Synthesis and biological evaluation of anti-Toxoplasma gondii activity of a novel scaffold of thiazolidinone derivatives

Simone Carradori, Daniela Secci, Bruna Bizzarri, Paola Chimenti, Celeste De Monte, Paolo Guglielmi, Cristina Campestre, Daniela Rivanera, Claudia Bordón, Lorraine Jones-Brando

Research output: Contribution to journalArticlepeer-review

Abstract

We designed and synthesised novel N-substituted 1,3-thiazolidin-4-one derivatives for the evaluation of their anti-Toxoplasma gondii efficacy. This scaffold was functionalised both at the N1-hydrazine portion with three structurally different moieties and at the lactam nitrogen with substituted benzyl groups selected on the basis of our previous structure-activity relationships studies. Using three different assay methods, the compounds were assessed in vitro to determine both the levels of efficacy against the tachyzoites of T. gondii (IC50 = 5–148 μM), as well as any evidence of cytotoxicity towards human host cells (TD50 = 68 to ≥320 μM). Results revealed that ferrocene-based thiazolidinones can possess potent anti-tachyzoite activity (TI =2–64).

Original languageEnglish (US)
Pages (from-to)746-758
Number of pages13
JournalJournal of Enzyme Inhibition and Medicinal Chemistry
Volume32
Issue number1
DOIs
StatePublished - Jan 1 2017

Keywords

  • 1,3-thiazolidin-4-one
  • Toxoplasma
  • cytotoxicity
  • ferrocene
  • host cell invasion
  • parasite growth inhibition

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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