title: Nontoxic Metal-Cyclam Complexes, a New Class of Compounds with Potency against Drug-Resistant Mycobacterium tuberculosis.
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.
authors.affiliation: School of Chemistry, The University of Sydney , Sydney, NSW 2006, Australia.
authors.forename: Mingfeng
authors.initials: M
authors.lastname: Yu
authors.affiliation: Microbial Immunity and Pathogenesis Group, Department of Infectious Diseases and Immunology, Sydney Medical School, The University of Sydney , Sydney, NSW 2006, Australia.
authors.forename: Gayathri
authors.initials: G
authors.lastname: Nagalingam
authors.affiliation: Microbial Immunity and Pathogenesis Group, Department of Infectious Diseases and Immunology, Sydney Medical School, The University of Sydney , Sydney, NSW 2006, Australia.
authors.forename: Samantha
authors.initials: S
authors.lastname: Ellis
authors.affiliation: Centre for Infectious Diseases and Microbiology Laboratory Services, Institute of Clinical Pathology and Medical Research-Pathology West, Westmead Hospital, Westmead, NSW 2145, Australia.
authors.forename: Elena
authors.initials: E
authors.lastname: Martinez
authors.affiliation: Centre for Infectious Diseases and Microbiology Laboratory Services, Institute of Clinical Pathology and Medical Research-Pathology West, Westmead Hospital, Westmead, NSW 2145, Australia.
authors.forename: Vitali
authors.initials: V
authors.lastname: Sintchenko
authors.affiliation: School of Chemistry, The University of Sydney , Sydney, NSW 2006, Australia.
authors.forename: Malcolm
authors.initials: M
authors.lastname: Spain
authors.affiliation: School of Chemistry, The University of Sydney , Sydney, NSW 2006, Australia.
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Rutledge
authors.affiliation: School of Chemistry, The University of Sydney , Sydney, NSW 2006, Australia.
authors.forename: Matthew H
authors.initials: MH
authors.lastname: Todd
authors.affiliation: Microbial Immunity and Pathogenesis Group, Department of Infectious Diseases and Immunology, Sydney Medical School, The University of Sydney , Sydney, NSW 2006, Australia.
authors.forename: James A
authors.initials: JA
authors.lastname: Triccas
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D006801:Humans; D051379:Mice; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D008968:Molecular Conformation; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000254:growth & development; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D018088:Tuberculosis, Multidrug-Resistant / Q000188:drug therapy*
chemical_list: D000995:Antitubercular Agents; D009942:Organometallic Compounds