Abstract

DARREL, Oliver T. et al. Synthesis, Antiplasmodial and Antitrypanosomal Evaluation of a Series of Novel 2-Oxoquinoline-based Thiosemicarbazone Derivatives. S.Afr.j.chem. (Online) [online]. 2018, vol.71, pp.174-181. ISSN 1996-840X.  http://dx.doi.org/10.17159/0379-4350/2018/v71a23.

Herein a series of novel thiosemicarbazones (TSCs) derived from 2-oxoquinoline scaffold is reported, and the target compounds have been successfully synthesized and characterized using standard spectroscopic techniques. The in vitro biological activities of synthesized molecules were evaluated against Plasmodium falciparum malaria parasites (strain 3D7), Trypanosoma brucei brucei parasites (strain 427) and HeLa cells. All the compounds displayed modest or no activity at a concentration of 20 μΜ and percentage viability of >50 % was often observed. Except for compound 9o, none of the final compounds exhibited cytotoxic effects against HeLa cells at 20 μΜ.

Keywords : Trypanosoma brucei; trypanosomiasis; Plasmodium falciparum; thiosemicarbazones; 2-oxoquinoline.

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