Tuberculosis (TB) is a bacterial disease infecting over 2 billion people and is caused by Mycobacterium tuberculosis (M. tb). HTS identified a number of novel scaffolds with antitubercular activity. Here we report the medicinal chemistry efforts on a scaffold leading to highly active small molecules with low nanomolar activity against M. tb in vitro and very low general cytotoxicity.

Discovery and development of highly potent inhibitors of <i>Mycobacterium tuberculosis</i> growth in vitro

243rd National Meeting (2012)

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Discovery and development of highly potent inhibitors of Mycobacterium tuberculosis growth in vitro