Application of aromatic ester compounds in preparing anti-enterovirus 71-type medicine
A technology of ester compounds and enteroviruses, applied in antiviral agents, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of biological activity evaluation, etc., and achieve low price, easy purchase, and easy The effect of mass production promotion
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Embodiment 1
[0022] [Example 1] Synthesis of novel aromatic ester compounds
[0023] The present invention has synthesized the following six novel aromatic ester compounds, referring to the method of the literature Tetrahedron Letters2015, 56, 6136-6141, specifically using transition metal palladium as a catalyst, under the induction of the ortho position of pyridine, in the ortho position of the aromatic ring The role of hypervalent iodobenzene, aroyloxylation, to obtain the final esterification product.
[0024]
Embodiment 2
[0025] [Example 2] Evaluation of the anti-EV71 activity of six pyridine aromatic ester compounds
[0026] 1. Test method:
[0027] 1.1 Toxicity of compounds to host RD cells
[0028] Plate RD cells into 96-well plates at 37 °C, 5% CO 2 After the monolayer was grown in the incubator, the cell culture solution was discarded, and the cell maintenance solution containing different concentrations of the test compound was added to continue the culture. After 48 hours, the cytotoxicity was visually observed under the microscope and recorded respectively, and the cell survival rate was determined by the MTT method. SPSS 11.5 software calculates the median toxic concentration (Medencyctoxic concentration, CC50) of the drug on the cells. Cell viability=(average OD of drug group 492 Value / average OD of cell control group 492 value) × 100%.
[0029] 1.2 Inhibitory activity of compounds against EV71
[0030] Plate RD cells into 96-well plates at 37 °C, 5% CO 2 After the monolayer wa...
Embodiment 3
[0040] [Example 3] The inhibitory effect of WY112 on the production of EV71 progeny virus
[0041] 1. Test method
[0042] RD cells in the logarithmic growth phase were plated in 24-well plates, and 100TCID after the monolayer was overgrown 50 Cells were infected with EV71, incubated at 37°C for 1.5h, removed the virus solution, washed three times with PBS, and added cell maintenance solution containing 40μg / mL WY112. After 48 hours, the cells and supernatant were collected and lysed by freezing and thawing three times at -20°C and 37°C. TCID 50 Methods The titer of EV71 virus was determined.
[0043] 2. Test results
[0044] Such as image 3 As shown, compared with the virus control group, the virus titer of RD cells treated with 40 μg / mL WY112 was significantly decreased, indicating that the compound had a strong inhibitory effect on the production of EV71 progeny virus.
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