Evaluation of the antimicrobial activity of a pyrimidine compound 2-methyl-3-(2-phenyl-2-oxoethyl) quinazolin-4(3H)-on against Klebsiella pneumoniae under in vivo conditions
https://doi.org/10.29001/2073-8552-2023-38-1-175-180
Abstract
The greatest danger is the development of multiple antimicrobial resistance in microorganisms, including Klebsiella pneumoniae, which actualizes the necessity of development and synthesis of new antimicrobial compounds. Considering the versatile pharmacological activity, pyrimidine compounds became a subject of interest for scientists in the aspect of their use as a basis for new antimicrobial agents.
Aim: To assess the antimicrobial activity of the pyrimidine compound 2-Methyl-3-(2-phenyl-2-oxoethyl)quinazoline-4(3H)-on against Kl. pneumoniae under in vivo conditions.
Material and Methods. The antimicrobial activity in vivo of the compound 2-Methyl-3-(2-phenyl-2-oxoethyl)quinazolin-4(3H)-on against Kl. pneumoniae was performed simulating generalized infection by intraperitoneal injection of the pathogen at a dose of 3 × 106. The experiment was conducted on CBA line mice (40 animals) divided into groups: control I – animals received intraperitoneal injection water; control II – infected animals received no treatment; experimental groups – mice with generalized infection treated with ceftriaxone at the dose 50 mg/kg intraperitoneally for 7 days, and the animals receiving the test compound at the dose 27 mg/kg against infection in the same mode. Antimicrobial activity was assessed by the following parameters: animal survival rate; internal organ and blood infestation index; total leukocyte count, C-reactive protein and procalcitonin.
Results. It was found that pyrimidine derivative 2-Methyl-3-(2-phenyl-2-oxoethyl)quinazoline-4(3H)-on has a marked antimicrobial activity against Kl. pneumonia appeared in increase of animal survival in the conditions of generalized Klebsiella infection as well as in decrease of total leukocyte count, C-reactive protein and procalcitonin levels that confirms the reduction of the inflammatory reaction.
Conclusion. Thus, the pyrimidine derivative 2-Methyl-3-(2-phenyl-2-oxoethyl)quinazoline-4(3H)-on exhibits antimicrobial activity, comparable with ceftriaxone, against Klebsiella pneumoniae in experimental generalized Klebsiella infection.
Keywords
About the Authors
A. A. TsybizovaRussian Federation
Alexandra A. Tsybizova - Cand. Sci. (Pharm.), Associate Professor, Head of the Research Center; Associate Professor, Pharmacognosy, Pharmaceutical Technology and Biotechnology Chair, Astrakhan State Medical University.
121 Bakinskaya str., Astrakhan, 414000
A. L. Yasenyavskaya
Russian Federation
Anna L. Yasenyavskaya - Cand. Sci. (Med.), Associate Professor, Head of the Research Center; Associate Professor, Pharmacognosy, Pharmaceutical Technology and Biotechnology Chair, Astrakhan State Medical University.
121 Bakinskaya str., Astrakhan, 414000
I. N. Tyurenkov
Russian Federation
Ivan N. Tyurenkov - Dr. Sci. (Med.), Corresponding Member of RAS, Professor, Head of the Pharmacology and Pharmacy Chair, Institute of Continuing Medical and Pharmaceutical Education of the FAMT, Volgograd State Medical University.
1, Fallen Fighters sq., Volgograd, 400131
A. A. Ozerov
Russian Federation
Alexander A. Ozerov - Dr. Sci. (Chem.), Professor, Head of the Pharmaceutical and Toxicological Chemistry Chair, Volgograd State Medical University.
1, Fallen Fighters sq., Volgograd, 400131
M. A. Samotrueva
Russian Federation
Marina A. Samotrueva - Dr. Sci. (Med.), Professor, Head of the Pharmacognosy, Pharmaceutical Technology and Biotechnology Chair, Astrakhan State Medical University.
121 Bakinskaya str., Astrakhan, 414000
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Review
For citations:
Tsybizova A.A., Yasenyavskaya A.L., Tyurenkov I.N., Ozerov A.A., Samotrueva M.A. Evaluation of the antimicrobial activity of a pyrimidine compound 2-methyl-3-(2-phenyl-2-oxoethyl) quinazolin-4(3H)-on against Klebsiella pneumoniae under in vivo conditions. Siberian Journal of Clinical and Experimental Medicine. 2023;38(1):175-180. (In Russ.) https://doi.org/10.29001/2073-8552-2023-38-1-175-180