Drug Development Targeting KasA in M. tuberculosis

By Megan Baxter

Faculty Mentor: Davis Oldham


Tuberculosis is a highly infectious disease affecting the lungs and respiratory system caused by Mycobacterium tuberculosis (M. tuberculosis). As one of the most dangerous lung diseases, recent studies have found existing treatments to become resistant and call for new treatments. Research involving the inhibition of KasA (β-ketoacyl synthase), which is responsible for mycobacterial cell wall, has become appealing and a druggable target for treatment. Sulfonamide and amine derivatives fully synthesized help to prevent such elongation of the backbone and formation of fatty acids that make up the mycobacterial cell wall. A sequence of three reactions have been performed so far. 6-nitroindazole was alkylated to form 1-methy-l-6-nitroindazole which was reduced to 6-aminoindazole-1-methyl with iron. The resulting amino group was then converted to a sulfonamide with benzenesulfonyl chloride. Nuclear magnetic resonance (NMR) and thin magnetic chromatography (TLC) tests were conducted. Future plans consist of testing these solutions to display their efficiency against the inhibition of KasA.




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