Nontoxic Metal-Cyclam Complexes, a New Class of Compounds with Potency against Drug-Resistant Mycobacterium tuberculosis

作者：Yu Mingfeng; Nagalingam Gayathri; Ellis Samantha; Martinez Elena; Sintchenko Vitali; Spain Malcolm; Rutledge Peter J^*; Todd Matthew H; Triccas James A

来源：Journal of Medicinal Chemistry, 2016, 59(12): 5917-5921.

DOI：10.1021/acs.jmedchem.6b00432

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.

• 出版日期2016-6-23