INVESTIGATION OF THE ACTIVITY OF 1.3-DIAZINONE-4 NEW DERIVATIVES AND THEIR NON-CYCLIC PRECURSORS IN RESPECT OF ESCHERICHIA COLI
https://doi.org/10.19163/2307-9266-2018-6-1-73-85
Abstract
In various countries of the world, for at least last fifteen years, in the structure of nosocomial infections the leading position has been occupied by gram-negative pathogens, Escherichia coli in particular. The data of the World Health Organization testify the increasing resistance of this pathogen to antibiotics, which determines the relevance of creating and developing new antimicrobial agents. Primary screening of new 1.3-diazinon-4 derivatives and their non-cyclic precursors made it possible to identify the leader compounds capable of active suppressing the growth of E. coli and promising for the further study. The aim of the study is to investigate the activity of the compounds under laboratory ciphers of PYaTs4, PYaTs6, PYaTs7, PJTd8, PYaTd9, PYaTd15 with respect to Escherichia coli. Materials and methods. The study of the activity of the compounds was carried out on the basis of collection and freshly isolated strains from patients with different pathologies. Before the inoculation all the strains were identified by means of the BIOMIC V3 software complex (Giles Scientific, USA) to confirm their belonging to the genus and species. The strains used in the work were previously tested for susceptibility to antibacterial drugs by the disk method to assess the presence or absence of resistance. The activity of the new compounds was studied by the serial dilution method. Results and discussion. The investigation of the sensitivity of the strains by the disk method to antibacterial drugs used in the etiotropic therapy of infections caused by Escherichia coli revealed microorganisms with multiple drug resistance. The analysis of the inoculation of the strains showed that all the studied compounds have the ability to suppress the growth of E. coli being both collectively and freshly isolated from patients with various pathologies. Conclusion. The substances under the laboratory ciphers of PYaTd8 and PYaTs4 are the most active in respect to the studied strains. At the same time, the MIC50 (minimum inhibitory concentration) of all the compounds does not exceed 10–20 μg / ml, which makes them promising for the further study.
Keywords
About the Authors
S. A. LuzhnovaRussian Federation
PhD (Biology), senior science master of FSBI “Research Institute for the Study of Leprosy”. Research interests: search and development of substances of synthetic, vegetable, animal, mineral origin, possessing antibacterial activity; search for correctors for dapsone-induced disorders, optimization of anti-leprosy therapy
A. V. Voronkov
Russian Federation
PhD (Medicine), docent, head of the Department of pharmacology with a course of clinical pharmacology,Pyatigorsk Medical and Pharmaceutical Institute – branch of Volgograd State Medical University. Research interests: search for substances with endothelioprotective activity; development of ways of pharmacological correction of conditions arising in individuals experiencing constant extreme physical and psychoemotional stress, including sports of high achievements; legal aspects of sports medicine; innovative approaches in the sphere of postgraduate education specialists
I. P. Kodonidi
Russian Federation
PhD (Pharmacy), Professor of the Department of Organic Chemistry, Рyatigorsk Medical Pharmaceutical Institute of Volgograd Medical State University. Research interests: molecular design of biologically active compounds in the series of 4-oxopyrimidine and chinalazone-4 derivatives, a purposeful synthesis of the most promising compounds with anti-inflammatory, antihypoxic, cerebroprotective activity, and also influence on the central nervous system
N. M. Gabitova
Russian Federation
junior research fellow of FSBI “Research Institute for the Study of Leprosy”, Ministry of Health of Russia.Research interests: search and development of substances of synthetic, vegetable, animal, mineral origin, possessing antibacterial activity; microbiological monitoring of antibacterial activity of drugs, substances being developed
Suda Billel
Russian Federation
Postgraduate Student, Department of Pharmacology with a course of clinical pharmacology, Pyatigorsk Medical and Pharmaceutical Institute – branch of Volgograd State Medical University. Research interests: search for substances having antibacterial activity; study of acute and chronic toxicity of compounds
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Review
For citations:
Luzhnova S.A., Voronkov A.V., Kodonidi I.P., Gabitova N.M., Billel S. INVESTIGATION OF THE ACTIVITY OF 1.3-DIAZINONE-4 NEW DERIVATIVES AND THEIR NON-CYCLIC PRECURSORS IN RESPECT OF ESCHERICHIA COLI. Pharmacy & Pharmacology. 2018;6(1):73-85. (In Russ.) https://doi.org/10.19163/2307-9266-2018-6-1-73-85