期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 32, 期 1, 页码 746-758出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2017.1316494
关键词
Toxoplasma; parasite growth inhibition; host cell invasion; cytotoxicity; 1,3-thiazolidin 4-one; ferrocene
资金
- FILAS (Regione Lazio, Italy) [ASR2]
- Stanley Medical Research Institute
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).
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据