Quinoline hybrids and their antiplasmodial and antimalarial activities

被引:319
作者
Hu, Yuan-Qiang [1 ]
Gao, Chuan [2 ]
Zhang, Shu [3 ]
Xu, Lei [2 ]
Xu, Zhi [2 ]
Feng, Lian-Shun [2 ]
Wu, Xiang [2 ]
Zhao, Feng [2 ]
机构
[1] Hubei Engn Univ, Sch Chem & Mat Sci, Xiaogan, Hubei, Peoples R China
[2] WuXi AppTec Wuhan, Wuhan, Hubei, Peoples R China
[3] Pony Testing Int Grp Wuhan, Wuhan, Hubei, Peoples R China
关键词
Antiplasmodials; Antimalarials; Quinoline; Quinolone; N-contained heterocycles; Hybrids; Structure-activity relationship; ACTIVITY IN-VITRO; BETA-HEMATIN INHIBITION; RESISTANT PLASMODIUM-FALCIPARUM; DRUG-DEVELOPMENT CANDIDATE; ANTI-PNEUMOCYSTIS-CARINII; METAL-BASED CHEMOTHERAPY; CHLOROQUINE-RESISTANT; BIOLOGICAL EVALUATION; 4-AMINOQUINOLINE DERIVATIVES; SIDE-CHAIN;
D O I
10.1016/j.ejmech.2017.07.061
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Malaria, in particular infection with P. falciparum (the most lethal of the human malaria parasite species, responsible for nearly one million deaths every year), is one of the most devastating and common infectious disease throughout the world. Beginning with quinine, quinoline containing compounds have long been used in clinical treatment of malaria and remained the mainstays of chemotherapy against malaria. The emergence of P. falciparum strains resistant to almost all antimalarials prompted medicinal chemists and biologists to study their effective replacement with an alternative mechanism of action and new molecules. Combination with variety of quinolines and other active moieties may increase the antiplasmodial and antimalarial activities and reduce the side effects. Thus, hybridization is a very attractive strategy to develop novel antimalarials. This review aims to summarize the recent advances towards the discovery of antiplasmodial and antimalarial hybrids including quinoline skeleton to provide an insight for rational designs of more active and less toxic quinoline hybrids antimalarials. (C) 2017 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:22 / 47
页数:26
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