Nontoxic Metal–Cyclam Complexes, a New Class of Compounds with Potency against Drug-Resistant Mycobacterium tuberculosis
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- 作者：Mingfeng Yu ; Gayathri Nagalingam ; Samantha Ellis ; Elena Martinez ; Vitali Sintchenko ; Malcolm Spain ; Peter J. Rutledge ; Matthew H. Todd ; James A. Triccas
- 刊名：Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：June 23, 2016
- 年：2016
- 卷：59
- 期：12
- 页码：5917-5921
- 全文大小：311K
- 年卷期：0
- ISSN：1520-4804
文摘
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.