Non-toxic metal-cyclam complexes, a new class of compounds with potency against drug-resistant Mycobacterium tuberculosis
Access status:
Open Access
Type
ArticleAuthor/s
Yu, MingfengNagalingam, Gayathri
Ellis, Samantha
Martinez, Elena
Sintchenko, Vitali
Spain, Malcolm
Rutledge, Peter J
Todd, Matthew H
Triccas, James A.
Abstract
Tuberculosis (TB) accounted for 1.5 million deaths in 2014 and new classes of anti-TB drugs are required. We re-port a class of functionalized 1,8-disubstituted cyclam derivatives that display low micromolar activity against pathogenic myco-bacteria. These compounds inhibit intracellular growth of Mycobacterium tuberculosis, are non-toxic 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.Tuberculosis (TB) accounted for 1.5 million deaths in 2014 and new classes of anti-TB drugs are required. We re-port a class of functionalized 1,8-disubstituted cyclam derivatives that display low micromolar activity against pathogenic myco-bacteria. These compounds inhibit intracellular growth of Mycobacterium tuberculosis, are non-toxic 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.
See less
See less
Date
2016-05-23Publisher
American Chemical SocietyCitation
Yu, M., Nagalingam, G., Ellis, S., Martinez, E., Sintchenko, V., Spain, M., Rutledge, P., Todd, M., Triccas, J. (2016). Nontoxic metal-cyclam complexes, a new class of compounds with potency against drug-resistant Mycobacterium tuberculosis. Journal of Medicinal Chemistry, 59(12), 5917-5921Share