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Nitroimidazoles, Quinolones and Oxazolidinones as Fluorine Bearing Antitubercular Clinical Candidates

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    SYSNO ASEP0451018
    Document TypeJ - Journal Article
    R&D Document TypeJournal Article
    Subsidiary JČlánek ve WOS
    TitleNitroimidazoles, Quinolones and Oxazolidinones as Fluorine Bearing Antitubercular Clinical Candidates
    Author(s) Patel, Rahul V. (UEB-Q)
    Keum, Y.S. (KR)
    Park, S.W. (KR)
    Source TitleMini - Reviews in Medicinal Chemistry - ISSN 1389-5575
    Roč. 15, č. 14 (2015), s. 1174-1186
    Number of pages13 s.
    Languageeng - English
    CountryNL - Netherlands
    KeywordsAntitubercular drugs ; delamanid ; fluorine-containing drugs
    Subject RIVEB - Genetics ; Molecular Biology
    R&D ProjectsLO1204 GA MŠk - Ministry of Education, Youth and Sports (MEYS)
    Institutional supportUEB-Q - RVO:61389030
    UT WOS000362519700006
    DOI10.2174/1389557515666150709121153
    AnnotationTuberculosis is a leading killer of lives worldwide and the global curse of multi-drug resistant tuberculosis is attaining really dangerous levels. Synergistic interaction of HIV and TB is the twin epidemics in resource-limited countries as each potentiate progression of the other. The increasing emergence of MDR-TB and XDR-TB place an immense burden for the treatment of TB with currently available drugs. The situation urgently demands for the discovery of new drugs with novel mode of action and differs in structural features in order to overcome resistance appears in conventional TB therapeutics. The present report covers the discovery of three classes of antituberculosis drugs, Nitroimidazoles, Quinolones and Oxazolidinones, undergoing clinical development with fluorine atom in their structures. Highly electronegative fluorine atom plays a signature role in advancing medicinal innovations as it existence in the drug compounds critically influences metabolic stability and lipophilicity thereby delaying its elimination by the body which results into a long term in vivo efficiency of the drug. Presence of fluorine atom(s) in the drug structures described in this report, has been associated with the several fold increase in the overall potency of the compound as demonstrated since the early discoveries. 6 Fluorinated derivatives from these three classes as pretomanid, delamanid, moxifloxacin, gatifloxacin, linezolid and sutezolid have been discussed with their antituberculosis effects, mode of action, chemical synthetic routes and results of clinical studies.
    WorkplaceInstitute of Experimental Botany
    ContactDavid Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469
    Year of Publishing2016