Synthesis and biological evaluation of anti-Toxoplasma gondii activity of a novel scaffold of thiazolidinone derivatives.
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).
['Carradori|Simone|S|', 'Secci|Daniela|D|', 'Bizzarri|Bruna|B|', 'Chimenti|Paola|P|', 'De Monte|Celeste|C|', 'Guglielmi|Paolo|P|', 'Campestre|Cristina|C|', 'Rivanera|Daniela|D|', 'Bordón|Claudia|C|', 'Jones-Brando|Lorraine|L|']
D000981:Antiprotozoal Agents D004305:Dose-Response Relationship, Drug D015394:Molecular Structure D021261:Parasitic Sensitivity Tests D013329:Structure-Activity Relationship D053778:Thiazolidines D014122:Toxoplasma
1,3-thiazolidin-4-one cytotoxicity Toxoplasma ferrocene host cell invasion parasite growth inhibition