Synthesis and biological evaluation of anti-Toxoplasma gondii activity of a novel scaffold of thiazolidinone derivatives

被引：23

作者：

Carradori, Simone ^{[1
]}

Secci, Daniela ^{[2
]}

Bizzarri, Bruna ^{[2
]}

Chimenti, Paola ^{[2
]}

De Monte, Celeste ^{[2
]}

Guglielmi, Paolo ^{[2
]}

Campestre, Cristina ^{[1
]}

Rivanera, Daniela ^{[3
]}

Bordon, Claudia ^{[4
]}

Jones-Brando, Lorraine ^{[4
]}

机构：

[1] G DAnnunzio Univ Chieti Pescara, Dept Pharm, Chieti, Italy

[2] Sapienza Univ Rome, Dept Drug Chem & Technol, Ple A Moro 5, I-00185 Rome, Italy

[3] Sapienza Univ Rome, Dept Publ Hlth & Infect Dis, Rome, Italy

[4] Johns Hopkins Univ, Sch Med, Stanley Div Dev Neurovirol, Baltimore, MD USA

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2017年 / 32卷 / 01期

关键词：

Toxoplasma; parasite growth inhibition; host cell invasion; cytotoxicity; 1,3-thiazolidin 4-one; ferrocene; IN-VITRO; SCHIZOPHRENIA; INHIBITORS; DESIGN;

D O I：

10.1080/14756366.2017.1316494

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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).

引用

页码：746 / 758

页数：13

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