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EVALUATION OF ANTIBACTERIAL ACTIVITY OF HYBRID COMPOUNDS BETWEEN THREE- AND TWO-MEMBERED HETECYCLICS — INHIBITORS OF RNA SYNTHESIS

A. V. Vasylchenko1, D. P. Egorov2, O. S. Mankovska1, I.G. Truntseva1,

S. M. Grigoryeva3, V. G. Kostina1,L. G. Palchykovska1

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1Institute of Molecular Biology and Genetics, NAS of Ukraine

 

150 Zabolotnogo Str., Kyiv, 03680, Ukraine

 

2O. O. Bogomolets National Medical University Ministryof Health of Ukraine 34 p

 

rospekt Peremogy Str., Кyiv, 03057, Ukraine

 

3SI «L.V. Gromashevsky Institute of Epidemiology and Infectious Diseases

 

of AMS Ukraine» 5 Amosova Str., Кyiv, 03038, Ukraine

 

The current work aims to evaluate the antibacterial activity of hybrid compounds the inhibitors of RNA synthesis and their DNA-binding ability. Antibacterial activity of compounds against the clinical strains of bacteria Staphylococcus aureus, Enterococcus faecalis and Pseudomonas aureginosa was investigated by serial two-fold dilution method in a liquid medium. DNA binding ability of hybrid compounds was studied by the DNA migration through agarose gel assay. The significant concentration- and structural-dependent bactericidal action of hybrid compounds against Gram-positive pathogens was observed. The compound 6 [4-(1,3-benzoxazol-2-yl)-9H-thioxanthen-9-one], which inhibits both bacteria with MBC values of 7.6 μM was determined as the most effective. It was shown, that compounds 1 [1-(1H-benzimidazol-2-yl)phenazine ], 2 2 [4-(1H-benzimidazol-2-yl)acridin-9(10H)-one] and 4 [4-(1H-benzimidazol-2-yl)-9H-thioxanthen-9-one] are able to bind to DNA duplexes. It is suggested that the inhibition of phage T7RNApolymerase by compound 2 can occur due to its DNA-binding ability.

 

 

 

Key words: HYBRID COMPOUNDS, ANTIBACTERIAL ACTIVITY, INHIBITORS OF RNA SYNTHESES, DNA-BINDING ABILITY

 

 

 

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