Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antitubercular Agents / chemical synthesis
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Antitubercular Agents / chemistry
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Antitubercular Agents / pharmacology*
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Cell Line
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Dose-Response Relationship, Drug
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Humans
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Mice
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Microbial Sensitivity Tests
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Models, Molecular
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Molecular Conformation
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Mycobacterium tuberculosis / drug effects*
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Mycobacterium tuberculosis / growth & development
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Organometallic Compounds / chemical synthesis
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Organometallic Compounds / chemistry
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Organometallic Compounds / pharmacology*
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Structure-Activity Relationship
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Tuberculosis, Multidrug-Resistant / drug therapy*
Substances
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Antitubercular Agents
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Organometallic Compounds