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Infectious disease


DNA gyrase

In vitro and mouse studies identified a series of N-linked aminopiperidine DNA gyrase inhibitors that could help treat tuberculosis infection. In vitro, the aminopiperidines inhibited DNA gyrase via a mechanism from fluoroquinolone antibiotics. In Mycobacterium tuberculosis culture, the aminopiperidines killed both fluoroquinolone-sensitive and fluoroquinolone-resistant strains. In mouse models of acute and chronic tuberculosis infection, the aminopiperidines decreased bacterial burden in the lung compared with fluoroquinolone antibiotics or vehicle. Researchers did not disclose next steps, which could include testing the compounds in additional animal models of tuberculosis infection.

SciBX 7(24); doi:10.1038/scibx.2014.714
Published online June 19, 2014

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Hameed P, S. et al. J. Med. Chem.;
published online May 8, 2014;
Contact: Shahul Hameed P, AstraZeneca India Pvt. Ltd., Bangalore, India