Malaria is one of the most prevalent parasitic infections for mankind, with over 40% of the world’s population at risk for malaria. The effectiveness of current antimalarial therapies, even that of gold-standard antimalarial drugs (artemisinin-based combination treatments, ACTs), is under threat by the emergence of drug-resistant parasites. Therefore, there is a pressing need for new antimalarials. Our previous investigations demonstrated that 4-nitro-styrylquinoline analogue (NSQ) exhibited promising antimalarial activity and excellent selectivity. Herein, we report a part of our follow-up study on the relationship between structure (R1 and R2 groups located at position C6 and C4 respectively, as well as the absence of styryl moiety or double bond between quinoline scaffold and R3-substituted aromatic or heterocyclic ring ) and antimalarial activity of styrylquinoline, the aim of which was to identify new compounds with significantly enhanced activity over NSQ towards P. falciparum in vitro and murine P. berghei ANKA in vivo, holding the potential for the treatment of malaria.

Design, synthesis, and structural activity relationships of styrylquinoline derivatives as potent antimalarial agents

2019 Spring National Meeting

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