Inhibition of DNA Gyrase by Levofloxacin and Related Fluorine-Containing Heterocyclic Compounds / Tunitskaya V. L.,Khomutov A. R.,Kochetkov S. N.,Kotovskaya S. K.,Charushin V. N. // ACTA NATURAE. - 2011. - V. 3, l. 4. - P. 94-99.

ISSN/EISSN:

2075-8251 / нет данных

Type:

Article

Abstract:

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.

Author keywords:

fluoroquinolones; levofloxacin; derivatives; bacterial DNA gyrase; enzymatic activity; inhibition KINETIC RESOLUTION; CHLORIDE; (+/-)-2,3-DIHYDRO-3-METHYL-4H-1,4-BENZOXAZINE; (S)-NAPROXEN; AMINES

DOI:

нет данных

Web of Science ID:

ISI:000309952100010

Соавторы в МНС:

Другие поля

Поле	Значение
Month	OCT-DEC
Publisher	RUSSIAN FEDERATION AGENCY SCIENCE \& INNOVATION
Address	NAUCHNY PARK MGU, VLAD 1, STROENIYE 75G, LENINSKIYE GORY, MOSCOW, 119991, RUSSIA
Language	English
Keywords-Plus	KINETIC RESOLUTION; CHLORIDE; (+/-)-2,3-DIHYDRO-3-METHYL-4H-1,4-BENZOXAZINE; (S)-NAPROXEN; AMINES
Research-Areas	Biochemistry \& Molecular Biology; Cell Biology
Web-of-Science-Categories	Biochemistry \& Molecular Biology; Cell Biology
Author-Email	ve\_tun@mail.ru
ResearcherID-Numbers	Kochetkov, Sergey /O-1065-2013
Funding-Acknowledgement	Federal Target Scientific and Technical Program ``Research and Development in Priority Areas of Science and Technology for{''} {[}02.522.12.2011]
Funding-Text	This work was supported by the Federal Target Scientific and Technical Program ``Research and Development in Priority Areas of Science and Technology for 2007-2013{''} (Government Contract No 02.522.12.2011).
Number-of-Cited-References	20
Usage-Count-Since-2013	2
Journal-ISO	Acta Naturae
Doc-Delivery-Number	022IS