- Klíčová slova
- benznidazol, Abarax,
- MeSH
- Chagasova nemoc * farmakoterapie MeSH
- lidé MeSH
- nitroimidazoly * aplikace a dávkování farmakologie terapeutické užití MeSH
- schvalování léčiv MeSH
- Check Tag
- lidé MeSH
Tuberculosis 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.
- MeSH
- antituberkulotika chemická syntéza chemie farmakologie MeSH
- chinolony chemická syntéza chemie farmakologie MeSH
- fluor chemie MeSH
- lidé MeSH
- nitroimidazoly chemická syntéza chemie farmakologie MeSH
- objevování léků MeSH
- oxazolidinony chemická syntéza chemie farmakologie MeSH
- tuberkulóza farmakoterapie MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- přehledy MeSH
- MeSH
- acetamidy farmakologie MeSH
- adamantan analogy a deriváty farmakologie MeSH
- antituberkulotika * farmakologie MeSH
- diarylchinoliny farmakologie MeSH
- ethylendiaminy farmakologie MeSH
- fluorochinolony farmakologie MeSH
- klinické zkoušky jako téma MeSH
- levofloxacin farmakologie MeSH
- lidé MeSH
- multirezistentní tuberkulóza farmakoterapie MeSH
- nitroimidazoly farmakologie MeSH
- oxazolidinony farmakologie MeSH
- oxazoly farmakologie MeSH
- racionální návrh léčiv MeSH
- rozvrh dávkování léků MeSH
- spirosloučeniny farmakologie MeSH
- thiaziny farmakologie MeSH
- tuberkulóza * farmakoterapie MeSH
- Check Tag
- lidé MeSH
- mužské pohlaví MeSH
- ženské pohlaví MeSH
- Publikační typ
- přehledy MeSH
- MeSH
- antibakteriální látky farmakologie MeSH
- Helicobacter pylori účinky léků MeSH
- laktamy MeSH
- nitroimidazoly farmakologie MeSH
- Publikační typ
- přehledy MeSH
