Synthesis and biological evaluation of anti-Toxoplasma gondii activity of a novel scaffold of thiazolidinone derivatives. (1st January 2017)

• Record Type: Journal Article
• Authors: Carradori, Simone; Secci, Daniela; Bizzarri, Bruna; Chimenti, Paola; De Monte, Celeste; Guglielmi, Paolo; Campestre, Cristina; Rivanera, Daniela; Bordón, Claudia; Jones-Brando, Lorraine
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 32:Number 1(2017)
• Page Start: 746
• Page End: 758
• Publication Date: 2017-01-01
• Subjects: Toxoplasma -- parasite growth inhibition -- host cell invasion -- cytotoxicity -- 1, 3-thiazolidin-4-one -- ferrocene; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.1080/14756366.2017.1316494
• Languages: English
• ISSNs: 1475-6366

Abstract

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).