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Updated: Mar 26, 2026

System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis
Published on: April 5, 2017
Synthesis and anti-tuberculosis activity of glycitylamines
Hilary M Corkran1, Emma M Dangerfield1, Gregory W Haslett2
1School of Chemical and Physical Sciences, Victoria University of Wellington, PO Box 600, 6140 Wellington, New Zealand; Malaghan Institute of Medical Research, PO Box 7060, Wellington, New Zealand.
Abstract:
A series of glycitylamines, which were prepared in few steps from readily available carbohydrates, were tested for their ability to inhibit tuberculosis growth in an Alamar Blue BCG colourimetric assay. Several derivatives, including (2R,3R)-1-(hexadecylamine)pent-4-ene-2,3-diol, (2R,3R)-1-(hexadecylmethylamino)pent-4-ene-2,3-diol and 5-deoxy-5-hexadecylmethylamino-D-arabinitol, were prepared in good to excellent (44-90%) overall yield and exhibited micromolar (20-41μM) inhibitory activity that was similar to the first line tuberculosis (TB) drug ethambutol (39μM) in the same assay. The ease and low cost of the synthesis of the glycitylamines offers definite advantages for their use as potential TB drugs.
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