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Publication: New quinolone-based thiosemicarbazones showing activity against plasmodium falciparum and Mycobacterium tuberculosis
Beteck, R.M Seldon, R Jordaan, A Warner, D.F Hoppe, H.C Laming, D Khanye, S.D
Beteck, R.M
Seldon, R
Jordaan, A
Warner, D.F
Hoppe, H.C
Laming, D
Khanye, S.D
Abstract
Co-infection of malaria and tuberculosis, although not thoroughly investigated, has been noted. With the increasing prevalence of tuberculosis in the African region, wherein malaria is endemic, it is intuitive to suggest that the probability of co-infection with these diseases is likely to increase. To avoid the issue of drug-drug interactions when managing co-infections, it is imperative to investigate new molecules with dual activities against the causal agents of these diseases. To this effect, a small library of quinolone-thiosemicarbazones was synthesised and evaluated in vitro against Plasmodium falciparum and Mycobacterium tuberculosis, the causal agents of malaria and tuberculosis, respectively. The compounds were also evaluated against HeLa cells for overt cytotoxicity. Most compounds in this series exhibited activities against both organisms, with compound 10, emerging as the hit; with an MIC90 of 2 µM against H37Rv strain of M. tuberculosis and an IC50 of 1 µM against the 3D7 strain of P. falciparum. This study highlights quinolone-thiosemicarabazones as a class of compounds that can be exploited further in search of novel, safe agents with potent activities against both the causal agents of malaria and tuberculosis.
Description
Date
2019-05-04
Journal Title
Journal ISSN
Volume Title
Publisher
MDPI
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Research Projects
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Keywords
Co-infections,Mycobacterium tuberculosis,Malaria,Quinolones,Thiosemicarbazones
Citation
Beteck RM, Seldon R, Jordaan A, et al. New quinolone-based thiosemicarbazones showing activity against plasmodium falciparum and Mycobacterium tuberculosis. Molecules. 2019 May 4;24(9):1740. doi: 10.3390/molecules24091740