Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 59, Issue 12, Pages 5917-5921Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b00432
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Funding
- National Health and Medical Research Council (NHMRC) [APP1084266]
- NHMRC Center of Research Excellence in Tuberculosis Control [APP1043225]
- University of Sydney Sydnovate Fund
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Tuberculosis (TB) accounted for 1.5 million deaths in 2014, and new classes of anti-TB drugs are required. We report a class of functionalized 1,8-disubstituted cyclam derivatives that display low micromolar activity against pathogenic mycobacteria. These compounds inhibit intracellular growth of Mycobacterium tuberculosis, are nontoxic to human cell lines, and are active against multidrug-resistant M. tuberculosis strains, indicating a distinct mode of action. These compounds warrant further appraisal as novel agents to control TB in humans.
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