Tuberculosis (TB) is a deadly global infection that has recently surpassed HIV/AIDS. ~250,000 of &gt;1 million deaths were from multidrug-resistant (MDR) TB, with only ~50% success in treatment of MDR-TB. Unless new strategies to combat or prevent emergence of drug-resistant TB are found, the global spread of MDR-TB will be an epidemic of epic proportions. Kanamycin A (KAN) is an antibiotic of last resort used to treat MDR-TB. Resistance to KAN signifies extensively drug-resistant (XDR) TB, which is nearly incurable. One-third of KAN-resistant TB is caused by upregulation of the acetyltransferase Eis in Mycobacteriumtuberculosis (Mtb), caused by mutations in the eispromoter. We investigated the mechanism of Eis and discovered and validated several Eis inhibitor scaffolds. In this presentation, the discovery and development of compounds to combat tuberculosis will be presented: (1) new Eis inhibitors as KAN adjuvants, and (2) new stand-alone agents active against Mtb. Medicinal chemistry optimization, activity, structural, and preliminary animal studies will be presented.

Novel compounds towards overcoming resistance in tuberculosis

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.