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 mu M), as well as any evidence of cytotoxicity towards human host cells (TD50 = 68 to >= 320 mu M). Results revealed that ferrocene-based thiazolidinones can possess potent antitachyzoite activity (TI = 2-64).

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

CARRADORI, Simone;CAMPESTRE, Cristina;
2017-01-01

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 mu M), as well as any evidence of cytotoxicity towards human host cells (TD50 = 68 to >= 320 mu M). Results revealed that ferrocene-based thiazolidinones can possess potent antitachyzoite activity (TI = 2-64).
File in questo prodotto:
File Dimensione Formato  
Synthesis and biological evaluation of anti Toxoplasma gondii activity of a novel scaffold of thiazolidinone derivatives (1).pdf

Solo gestori archivio

Tipologia: PDF editoriale
Dimensione 3.47 MB
Formato Adobe PDF
3.47 MB Adobe PDF   Visualizza/Apri   Richiedi una copia

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11564/669039
Citazioni
  • ???jsp.display-item.citation.pmc??? 5
  • Scopus 22
  • ???jsp.display-item.citation.isi??? 22
social impact