| Autor: |
Carradori, Simone, Secci, Daniela, Bizzarri, Bruna, Chimenti, Paola, Monte, Celeste De, Guglielmi, Paolo, Campestre, Cristina, Rivanera, Daniela, Bordón, Claudia, Jones-Brando, Lorraine |
| Rok vydání: |
2017 |
| DOI: |
10.6084/m9.figshare.5549602 |
| Popis: |
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). |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
|
