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作为对氯喹耐药恶性疟原虫菌株有效的抗疟药的N1-亚芳基-N2-喹啉基和N2-吖啶基腙的合成。

Synthesis of N1-arylidene-N2-quinolyl- and N2-acrydinylhydrazones as potent antimalarial agents active against CQ-resistant P. falciparum strains.

作者信息

Gemma Sandra, Kukreja Gagan, Fattorusso Caterina, Persico Marco, Romano Maria P, Altarelli Maria, Savini Luisa, Campiani Giuseppe, Fattorusso Ernesto, Basilico Nicoletta, Taramelli Donatella, Yardley Vanessa, Butini Stefania

机构信息

Dipartimento Farmaco Chimico Tecnologico, Università di Siena, via Aldo Moro, 53100 Siena, Italy.

出版信息

Bioorg Med Chem Lett. 2006 Oct 15;16(20):5384-8. doi: 10.1016/j.bmcl.2006.07.060. Epub 2006 Aug 4.

DOI:10.1016/j.bmcl.2006.07.060
PMID:16890433
Abstract

A series of N1-arylidene-N2-quinolyl- and N2-acrydinylhydrazones were synthesized and tested for their antimalarial properties. These compounds showed remarkable anti-plasmodial activity in vitro especially against chloroquine-resistant strains. Their potent biological activity makes them promising lead structures for the development of new antimalarial drugs.

摘要

合成了一系列N1-亚芳基-N2-喹啉基和N2-吖啶基腙，并对其抗疟性能进行了测试。这些化合物在体外显示出显著的抗疟原虫活性，尤其是对氯喹耐药菌株。它们强大的生物活性使其成为开发新型抗疟药物的有前景的先导结构。

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