title: In vitro and ex vivo activity of thioridazine derivatives against Mycobacterium tuberculosis.
abstract: Thioridazine (TZ) has previously been shown by us to have in vitro and ex vivo activity against antibiotic-susceptible and multidrug-resistant Mycobacterium tuberculosis (MDRTB). Because current therapy of MDRTB is highly problematic even when all five 'first line of defence' drugs are employed, there is a need for effective antituberculosis drugs. New derivatives of TZ were synthesised and their in vitro activity against a reference strain of M. tuberculosis was evaluated with the aid of the BACTEC 460 system. Derivatives that presented significant activity were evaluated by ex vivo studies and were shown to enhance the killing of intracellular M. tuberculosis.
authors.affiliation: Unidade de Micobacterias, UPMM, Instituto de Higiene e Medicina Tropical, Universidade de Lisboa, Rua da Junqueira 96, 1394-008 Lisbon, Portugal.
authors.forename: Marta
authors.initials: M
authors.lastname: Martins
authors.forename: Zsuzsanna
authors.initials: Z
authors.lastname: Schelz
authors.forename: Ana
authors.initials: A
authors.lastname: Martins
authors.forename: Joseph
authors.initials: J
authors.lastname: Molnar
authors.forename: Gyorgy
authors.initials: G
authors.lastname: Hajös
authors.forename: Zsuzsanna
authors.initials: Z
authors.lastname: Riedl
authors.forename: Miguel
authors.initials: M
authors.lastname: Viveiros
authors.forename: Ismail
authors.initials: I
authors.lastname: Yalcin
authors.forename: Esin
authors.initials: E
authors.lastname: Aki-Sener
authors.forename: Leonard
authors.initials: L
authors.lastname: Amaral
mesh_terms: D000995:Antitubercular Agents / Q000494:pharmacology*; D024901:Drug Resistance, Multiple, Bacterial; D006801:Humans; D066298:In Vitro Techniques; D008264:Macrophages / Q000382:microbiology; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D010587:Phagocytosis; D013881:Thioridazine / Q000031:analogs & derivatives* / Q000494:pharmacology
chemical_list: D000995:Antitubercular Agents; D013881:Thioridazine