Acta NaturaeActa NaturaeActa Naturae2075-8251Acta Naturae Ltd1066010.32607/20758251-2011-3-4-94-99ArticlesСтатьиResearch ArticleInhibition of DNA Gyrase by Levofloxacin and Related Fluorine-Containing Heterocyclic CompoundsInhibition of DNA Gyrase by Levofloxacin and Related Fluorine-Containing Heterocyclic CompoundsTunitskayaV Lve_tun@mail.ruKhomutovA RKochetkovS NKotovskayaS KCharushinV NEngelhardt Institute of Molecular Biology, Russian Academy of SciencesPostovsky Institute of Organic Synthesis, Ural Branch, Russian Academy of SciencesUrals Federal UniversityPostovsky Institute of Organic Synthesis, Ural Branch, Russian Academy of SciencesUrals Federal University1512201134VOL 3, NO4 (2011)ТОМ 3, №4 (2011)949917012020Copyright ©; 2011, Tunitskaya V.L., Khomutov A.R., Kochetkov S.N., Kotovskaya S.K., Charushin V.N.Copyright ©; 2011, Tunitskaya V.L., Khomutov A.R., Kochetkov S.N., Kotovskaya S.K., Charushin V.N.2011Tunitskaya V.L., Khomutov A.R., Kochetkov S.N., Kotovskaya S.K., Charushin V.N.Tunitskaya V.L., Khomutov A.R., Kochetkov S.N., Kotovskaya S.K., Charushin V.N.https://creativecommons.org/licenses/by/4.0https://actanaturae.ru/2075-8251/article/view/10660

Fluoroquinolones are an important class of modern and efficient antibacterial drugs with a broad spectrum of activity. Levofloxacin (the optically active form of ofloxacin) is one of the most promising fluoroquinolone drugs, and its antibacterial activity is substantially higher than the activity of other drugs of the fluoroquinolone family. Earlier, in the Postovsky Institute of Organic Synthesis, UB RAS, an original method of levofloxacin synthesis was developed, and now the pilot batch of the drug is being prepared. Bacterial DNA gyrase is a specific target of fluoroquinolones; hence, the study of the enzyme-drug interaction is of theoretical and practical importance. Moreover, the parameters of DNA gyrase inhibition may serve as a criterion for drug quality. Here, we present the results of studying the interaction of DNA gyrase with a number of fluoroquinolones and their analogs: intermediates and semi-products of the levofloxacin synthesis, and also samples from the pilot batches of this drug. The importance of two structural elements of the levofloxacin molecule for the efficiency of the inhibition is revealed. The data obtained may be useful for the design of new drugs derived from levofloxacin.

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