|
|||||
|
|
Activity of 7-methyljuglone derivatives against Mycobacterium tuberculosis and as subversive substrates for mycothiol disulfide reductase |
|
| Authors: | Mahapatra Anita Mativandlela Sannah P N Binneman B Fourie P B Hamilton Chris J Meyer J J M van der Kooy F Houghton Peter Lall Namrita |
| Institution: | aDepartment of Botany, Faculty of Natural and Agricultural Sciences, University of Pretoria, Pretoria 0002, South Africa bMedical Research Council, Pretoria, South Africa cSchool of Chemistry and Chemical Engineering, David Keir Building, Queen’s University Belfast, Stranmillis Road, Belfast BT9 5AG, UK dDepartment of Pharmacy, Franklin-Wilkins Building, 150 Stamford Street, King’s College London, London SE1 9NN, UK |
| 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). |
| Keywords: | Naphthoquinones Subversive substrates Disulfide reductase Mycothiol Tuberculosis |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |