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Synthesis, antiplasmodial and antitrypanosomal evaluation of a series of novel 2-oxoquinoline-based thiosemicarbazone derivatives


Oliver T. Darrell
Siyabonga T. Hulushe
Thanduxolo E. Mtshare
Richard M. Beteck
Michelle Isaacs
Dustin Laming
Heinrich C. Hoppe
Rui W.M. Krause
Setshaba D. Khanye

Abstract

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 μM 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 μM.

Keywords: Trypanosoma brucei, trypanosomiasis, Plasmodium falciparum, thiosemicarbazones, 2-oxoquinoline


Journal Identifiers


eISSN: 1996-840X
print ISSN: 0379-4350