Tuberculosis is one of the top ten causes of death in the world and is most prevalent in developing countries. Existing treatment protocols are problematic in that some strains of Mycobacterium tuberculosis have developed resistance. The DXR enzyme of the MEP pathway for the biosynthesis of isoprenoids, present in many eubacteria has recently been the target for the development of novel anti-microbials. Mycobacteria cells, such as M. tuberculosis, are surrounded by a hydrophobic, waxy cell wall and therefore they are resistant to known inhibitors of DXR due to the lack of uptake of such hydrophobic compounds. To circumvent this problem, we report the synthesis of a prodrug, a compound in which the phosphate moiety is masked. The prodrug was tested on non-pathogenic mycobacteria, Mycobacterium smegmatis.

Prodrug syntheses of an inhibitor of the deoxyxyulose reductoisomerase (DXR): A potential new antitubercular drug

255th National Meeting (2018)

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