Open AccessNontoxic Metal–Cyclam Complexes, a New Class of Compounds with Potency against Drug-Resistant Mycobacterium tuberculosis
Author(s) -
Mingfeng Yu,
Gayathri Nagalingam,
Samantha Ellis,
Elena Martínez,
Vitali Sintchenko,
Malcolm Spain,
Peter J. Rutledge,
Matthew H. Todd,
James A. Triccas
Publication year - 2016
Publication title -
journal of medicinal chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.01
H-Index - 261
eISSN - 1520-4804
pISSN - 0022-2623
DOI - 10.1021/acs.jmedchem.6b00432
Subject(s) - mycobacterium tuberculosis , chemistry , tuberculosis , mycobacterium smegmatis , potency , cyclam , drug , mycobacterium , drug resistance , mode of action , intracellular , microbiology and biotechnology , structure–activity relationship , in vitro , combinatorial chemistry , pharmacology , biochemistry , metal , biology , medicine , organic chemistry , pathology
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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