Ricerc@Sapienza

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