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喹啉类抗疟药的结构修饰:最新进展

Structural modifications of quinoline-based antimalarial agents: Recent developments.

作者信息

Bawa Sandhya, Kumar Suresh, Drabu Sushma, Kumar Rajiv

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi-110 062, India.

出版信息

J Pharm Bioallied Sci. 2010 Apr;2(2):64-71. doi: 10.4103/0975-7406.67002.

Abstract

Antimalarial drugs constitute a major part of antiprotozoal drugs and have been in practice for a long time. Antimalarial agents generally belong to the class of quinoline which acts by interfering with heme metabolism. The recent increase in development of chloroquine-resistant strains of Plasmodium falciparum and failure of vaccination program against malaria have fuelled the drug discovery program against this old and widespread disease. Quinoline and its related derivative comprise a class of heterocycles, which has been exploited immensely than any other nucleus for the development of potent antimalarial agents. Various chemical modifications of quinoline have been attempted to achieve analogs with potent antimalarial properties against sensitive as well as resistant strains of Plasmodium sp., together with minimal potential undesirable side effects. This review outlines essentially some of the recent chemical modifications undertaken for the development of potent antimalarial agents based on quinoline.

摘要

抗疟药物是抗原虫药物的主要组成部分,并且已经应用了很长时间。抗疟药一般属于喹啉类,其作用是干扰血红素代谢。近年来,恶性疟原虫氯喹耐药菌株的增加以及疟疾疫苗接种计划的失败,推动了针对这种古老且广泛传播疾病的药物研发计划。喹啉及其相关衍生物构成了一类杂环化合物,在开发强效抗疟药物方面,它比任何其他核心结构都得到了更广泛的应用。人们尝试了喹啉的各种化学修饰,以获得对疟原虫敏感株和耐药株均具有强效抗疟特性且潜在不良副作用最小的类似物。本综述主要概述了基于喹啉开发强效抗疟药物的一些近期化学修饰。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a96/3147106/7573f30d8258/JPBS-2-64-g001.jpg

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