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Hybrid molecules with potential in vitro antiplasmodial and in vivo antimalarial activity against drug‐resistant Plasmodium falciparum
Author(s) -
Feng LianShun,
Xu Zhi,
Chang Le,
Li Chuan,
Yan XiaoFei,
Gao Chuan,
Ding Chao,
Zhao Feng,
Shi Feng,
Wu Xiang
Publication year - 2020
Publication title -
medicinal research reviews
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.868
H-Index - 130
eISSN - 1098-1128
pISSN - 0198-6325
DOI - 10.1002/med.21643
Subject(s) - plasmodium falciparum , pharmacophore , malaria , in vivo , drug resistance , drug , pharmacology , chloroquine , biology , antimalarial agent , microbiology and biotechnology , immunology , bioinformatics
Abstract Malaria is a tropical disease, leading to around half a million deaths annually. Antimalarials such as quinolines are crucial to fight against malaria, but malaria control is extremely challenged by the limited pipeline of effective pharmaceuticals against drug‐resistant strains of Plasmodium falciparum which are resistant toward almost all currently accessible antimalarials. To tackle the growing resistance, new antimalarial drugs are needed urgently. Hybrid molecules which contain two or more pharmacophores have the potential to overcome the drug resistance, and hybridization of quinoline privileged antimalarial building block with other antimalarial pharmacophores may provide novel molecules with enhanced in vitro and in vivo activity against drug‐resistant (including multidrug‐resistant) P falciparum . In recent years, numerous of quinoline hybrids were developed, and their activities against a panel of drug‐resistant P falciparum strains were screened. Some of quinoline hybrids were found to possess promising in vitro and in vivo potency. This review emphasized quinoline hybrid molecules with potential in vitro antiplasmodial and in vivo antimalarial activity against drug‐resistant P falciparum , covering articles published between 2010 and 2019.