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4-酰基-2-噻唑基腙衍生物的合成及其体外抗弓形虫药效评价

Synthesis and evaluation of 4-acyl-2-thiazolylhydrazone derivatives for anti-Toxoplasma efficacy in vitro.

作者信息

Chimenti Franco, Bizzarri Bruna, Bolasco Adriana, Secci Daniela, Chimenti Paola, Carradori Simone, Granese Arianna, Rivanera Daniela, Frishberg Nathan, Bordón Claudia, Jones-Brando Lorraine

机构信息

Dipartimento di Chimica e Tecnologie del Farmaco, Università La Sapienza, P.le A. Moro 5, 00185 Rome, Italy.

出版信息

J Med Chem. 2009 Aug 13;52(15):4574-7. doi: 10.1021/jm9005862.

DOI:10.1021/jm9005862
PMID:19618935
Abstract

A new series of 4-acyl-2-thiazolylhydrazone derivatives was synthesized and screened for its in vitro activity against Toxoplasma gondii. We evaluated parasite growth inhibition and cytotoxicity, inhibition of replication, and inhibition of parasite invasion of host cells. The biological results indicated that some substances had an antiproliferative effect against intracellular T. gondii tachyzoites cultivated in vitro.

摘要

合成了一系列新的4-酰基-2-噻唑基腙衍生物,并对其抗刚地弓形虫的体外活性进行了筛选。我们评估了寄生虫生长抑制和细胞毒性、复制抑制以及寄生虫对宿主细胞侵袭的抑制。生物学结果表明,一些物质对体外培养的细胞内刚地弓形虫速殖子具有抗增殖作用。

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