Activity of 7-methyljuglone derivatives against Mycobacterium tuberculosis and as subversive substrates for mycothiol disulfide reductase
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Date
Authors
Mahapatra, Anita
Mativandlela, Sannah Patience Nkami
Binneman, Brigitte
Hamilton, Chris J.
Meyer, Jacobus Johannes Marion
Van der Kooy, Frank
Houghton, P.J. (Peter James)
Lall, Namrita
Journal Title
Journal ISSN
Volume Title
Publisher
Elsevier
Abstract
The naphthoquinone 7-methyljuglone (5-hydroxy-7-methyl-1,4-naphthoquinone) has previously been isolated and identified as an active component of root extracts of Euclea natalensis which displays antitubercular activity. Herein, a series of synthetic and plant-derived naphthoquinone derivates of the 7-methyljuglone scaffold have been prepared and evaluated for antibacterial activity against Mycobacterium tuberculosis. Several of these compounds have been shown to operate as subversive substrates with mycothiol disulfide reductase. The absence of a direct correlation between antitubercular activity and subversive substrate efficiency with mycothiol disulfide reductase, might be a consequence of their non-specific reactivity with multiple biological targets (e.g. other disulfide reductases).
Description
Keywords
Subversive substrates, Disulfide reductase, Mycothiol, Tuberculosis (TB)
Sustainable Development Goals
Citation
Mahapatra, A, Mativandlela, SPN, Binneman, B, Fourie, PB, Hamilton, CJ, Meyer, JJM, Van der Kooy, F, Houghton, P & Lall, N 2007, ‘Activity of 7-methyljuglone derivatives against Mycobacterium tuberculosis and as subversive substrates for mycothiol disulfide reductase’, Bioorganic & Medicinal Chemistry, vol.15, issue 24, pp. 7638-7646. [http://www.sciencedirect.com/science/journal/09680896]