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Article

New Quinolone-Based Thiosemicarbazones Showing Activity Against Plasmodium falciparum and Mycobacterium tuberculosis

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Division of Pharmaceutical Chemistry, Faculty of Pharmacy, Rhodes University, Grahamstown 6140, South Africa
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Drug Discovery and Development Centre (H3-D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa
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SAMRC/NHLS/UCT Molecular Mycobacteriology Research Unit, Department of Pathology, University of Cape Town, Observatory 7925, South Africa
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Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Observatory 7925, South Africa
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Wellcome Centre for Infectious Diseases Research in Africa, University of Cape Town, Observatory 7925, South Africa
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Department of Biochemistry and Microbiology, Faculty of Science, Rhodes University, Grahamstown 6140, South Africa
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Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa
*
Authors to whom correspondence should be addressed.
Molecules 2019, 24(9), 1740; https://doi.org/10.3390/molecules24091740
Received: 9 March 2019 / Revised: 4 April 2019 / Accepted: 9 April 2019 / Published: 4 May 2019
(This article belongs to the Section Medicinal Chemistry)
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. View Full-Text
Keywords: Co-infections; thiosemicarbazones; quinolones; malaria; Mycobacterium tuberculosis Co-infections; thiosemicarbazones; quinolones; malaria; Mycobacterium tuberculosis
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MDPI and ACS Style

Beteck, R.M.; Seldon, R.; Jordaan, A.; Warner, D.F.; Hoppe, H.C.; Laming, D.; Khanye, S.D. New Quinolone-Based Thiosemicarbazones Showing Activity Against Plasmodium falciparum and Mycobacterium tuberculosis. Molecules 2019, 24, 1740. https://doi.org/10.3390/molecules24091740

AMA Style

Beteck RM, Seldon R, Jordaan A, Warner DF, Hoppe HC, Laming D, Khanye SD. New Quinolone-Based Thiosemicarbazones Showing Activity Against Plasmodium falciparum and Mycobacterium tuberculosis. Molecules. 2019; 24(9):1740. https://doi.org/10.3390/molecules24091740

Chicago/Turabian Style

Beteck, Richard M., Ronnett Seldon, Audrey Jordaan, Digby F. Warner, Heinrich C. Hoppe, Dustin Laming, and Setshaba D. Khanye 2019. "New Quinolone-Based Thiosemicarbazones Showing Activity Against Plasmodium falciparum and Mycobacterium tuberculosis" Molecules 24, no. 9: 1740. https://doi.org/10.3390/molecules24091740

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