Abstract
It has been found that 6-[(b-dialkylaminoethylthio]-3-R-2H-[1,2,4]triazino[2,3-c]quinazolin-2-ones exhibit the antiviral activity against respiratory and the biodefence virus panel (EC50 3.2-36.0 mg/ml) and the influenza type A and B (EC50 1.1-18.0 mg/ml) in the visual (viral CPE) and neutral red dye uptake increasing tests. The high inhibitory activity of compound 1.5 against the strain Flu B (EC50 1.1-5.3 mg/ml) has been revealed. It has been suggested that the antiviral effect of compound 1.5 is comparable with Ribavirin. It has been shown that the planar [1,2,4]triazino[2,3-c]quinazoline system causes antiviral properties additionally determined by the b-dialkylaminoethylthiol fragment and depends on the nature of the substituent in position 3.
Highlights
The expansion of the mankind activity in the planet ecosystem causes the counter evolution of viruses specializing in exploiting the human organism resources
Our study describes the strategy for the synthesis of novel antiviral agents based on the “hybrid – pharmacophore” approach
Decrease in the virus yield assay (VYR-test) Compounds considered to be active by the cytopathic effect (CPE) inhibition and by the neutral red (NR) dye uptake were re-tested on reduction of the virus yield by assaying frozen and thawed eluates from each cup for the virus titre by serial dilution onto monolayers of susceptible cells
Summary
The expansion of the mankind activity in the planet ecosystem causes the counter evolution of viruses specializing in exploiting the human organism resources. Inhibition of the viral cytopathic effect (CPE) This test performed in 96 well flat-bottomed microplates was used for the initial antiviral evaluation of compounds. In this CPE inhibition test, four log dilutions of each test compound (e.g. 1000, 100, 10, 1 mg/ml) were added to 3 cups containing the cell monolayer within 5 min. Decrease in the virus yield assay (VYR-test) Compounds considered to be active by the CPE inhibition and by the NR dye uptake were re-tested on reduction of the virus yield by assaying frozen and thawed eluates from each cup for the virus titre by serial dilution onto monolayers of susceptible cells. The same as in the initial tests, a known active drug was used in parallel as a posi-
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