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合成 4-氨基喹啉类似物及其铂(II)配合物作为新型抗利什曼原虫和抗结核药物。

Synthesis of 4-aminoquinoline analogues and their platinum(II) complexes as new antileishmanial and antitubercular agents.

机构信息

Departamento de Química, ICE, Universidade Federal de Juiz de Fora, Campus Universitário, Juiz de Fora, MG 36036-900, Brazil.

出版信息

Biomed Pharmacother. 2011 Jun;65(3):204-9. doi: 10.1016/j.biopha.2011.01.003. Epub 2011 May 4.

Abstract

A series of 4-amino-7-chloroquinoline derivatives were synthesized by the reaction of 4,7-dichloro-quinoline with the corresponding diamine and then with propargyl bromide. In addition, platinum(II) complexes were obtained by reacting some of the organic derivatives with K(2)PtCl(4). Several of the synthesized compounds displayed antituberculosis activities. Compound 3 was 47.5 times more active than amphotericin B against Leishmania chagasi (IC(50)=0.04 μg/mL). Compounds 5, 6, 7, 9, 10, 11 and 13 presented promising results against Mycobacterium tuberculosis, with MIC values ranging from 12.5 to 15.6 μg/mL, comparable to the "first and second line" drugs used to treat tuberculosis.

摘要

一系列 4-氨基-7-氯喹啉衍生物是通过 4,7-二氯喹啉与相应的二胺反应,然后与丙炔溴反应合成的。此外,一些有机衍生物与 K(2)PtCl(4)反应得到铂(II)配合物。合成的几种化合物具有抗结核活性。化合物 3 对利什曼原虫(IC(50)=0.04 μg/mL)的活性比两性霉素 B 高 47.5 倍。化合物 5、6、7、9、10、11 和 13 对结核分枝杆菌表现出良好的效果,MIC 值在 12.5 到 15.6 μg/mL 之间,与用于治疗结核病的“一线和二线”药物相当。

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