Tuberculosis (TB) is a bacterial infection causes more deaths than any other infectious disease. It is estimated that 9 million people are infected with tuberculosis annually leading to an estimated 1.5 million deaths per year. Novel acrylic acid ethyl ester derivatives were synthesized and evaluated as potential agents against Mycobacterium species. Minimum inhibitory concentration (MIC) assays indicated that compounds 3 and 4 have in vitro activity against Mycobacterium smegmatis.  When tested against Mycobacterium tuberculosis and other Mycobacterium strains compounds 3 and 4 were found to have variable activity and SAR studies were started on this line of compounds.  Based on these studies two compounds were identified as potential leads, compounds 5 and 6 were found to have MICs of 8 �g/mL against Mycobacterium tuberculosis. SAR studies are ongoing and many derivatives of 5 and 6 are currently being tested for activity.

Design, synthesis, and SAR studies on a new class of antimycobacterials

245th National Meeting (2013)

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