Thiosemikarbazony a jejich antimykobakteriální účinky

Antimykobakteriální účinky thiosemikarbazonů byly objeveny ve druhé polovině čtyřicátých let 20. století. Nejznámějším zástupcem těchto sloučenin je thioacetazon používaný v terapii tuberkulózy od přelomu čtyřicátých a padesátých let. Pro závažné vedlejší účinky se dnes používá jen málokdy. Tato práce pojednává o antimykobakteriálních účincích thiosemikarbazonů a N,N-dimethylthiosemikarbazonů odvozených od 5-alkyl-2-acetylpyrazinů. Některé z těchto sloučenin významně inhibovaly růst Mycobacterium tuberculosis H₃₇Rv, ale pro svoji toxicitu nepostoupily do in vivo studií. Nicméně mohou být využity jako modelové sloučeniny pro studium mechanismů antimykobakteriálních účinků thiosemikarbazonů.

Klíčová slova:
tuberkulóza – thiosemikarbazony acetylpyrazinů – antimykobakteriální účinky

Autoři: Veronika Opletalová; Jan Doležel
Působiště autorů: Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Chemistry and Drug Analysis
Vyšlo v časopise: Čes. slov. Farm., 2013; 62, 78-83
Kategorie: Původní práce

Souhrn

Klíčová slova:
tuberkulóza – thiosemikarbazony acetylpyrazinů – antimykobakteriální účinky

Zdroje

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