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Application of nitrogen-containing heterocyclic aromatic ester compounds in the preparation of drugs against Coxsackie virus type b3

A technology of ester compounds and Coxsackie virus, applied in antiviral agents, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of biological activity evaluation, etc., and achieve rapid economical and easy large-scale production The effect of simple promotion and synthesis process

Active Publication Date: 2019-04-09
HUBEI UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Its biological activity has not been evaluated

Method used

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  • Application of nitrogen-containing heterocyclic aromatic ester compounds in the preparation of drugs against Coxsackie virus type b3
  • Application of nitrogen-containing heterocyclic aromatic ester compounds in the preparation of drugs against Coxsackie virus type b3
  • Application of nitrogen-containing heterocyclic aromatic ester compounds in the preparation of drugs against Coxsackie virus type b3

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] [Example 1] Synthesis of novel nitrogen-containing heterocyclic aromatic ester compounds

[0022] The present invention has synthesized the following 6 novel nitrogen-containing heterocyclic aromatic ester compounds, referring to the method of literature Tetrahedron Letters 2015, 56, 6136-6141, specifically using transition metal palladium as a catalyst, under the induction of the ortho position of pyridine, in the aromatic ring The ortho-position of aroyl is oxylated with hypervalent iodobenzene to obtain the final esterification product.

[0023]

Embodiment 2

[0024] [Example 2] Evaluation of the anti-CVB3 activity of 6 compounds

[0025] 1. Test method:

[0026] 1.1 Toxicity of compounds to host Hep-2 cells

[0027] Hep-2 cells were plated in 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 cytotoxic concentration (Median cyctoxic 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%.

[0028] 1.2 Inhibitory activity of compounds against CVB3

[0029] Hep-2 cells were plated in 96-well plates at 37°C, 5% CO 2 After the monolayer was gro...

Embodiment 3

[0039] [Example 3] The inhibitory effect of WY112 on the production of CVB3 progeny virus

[0040] 1. Test method

[0041] Hep-2 cells in the logarithmic growth phase were plated in 24-well plates, and 100TCID after the monolayer was overgrown 50 CVB3 infected cells, 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 culture fluid were collected, and after freezing and thawing three times at -20°C and 37°C, the titer of CVB3 virus was determined by the TCID50 method.

[0042] 2. Test results

[0043] Such as image 3 As shown, the virus titer of Hep-2 cells treated with 40 μg / mL WY112 was significantly lower than that of the virus control group, indicating that the compound had a strong inhibitory effect on the production of CVB3 progeny virus.

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Abstract

The invention belongs to the technical field of antiviral drugs, and relates to an application of novel nitrogenous heterocycle containing aromatic ester compounds WY92 and WY112 to preparation of a medicament for resisting Coxsaekievirus B3 type (CVB3). The compounds WY92 and WY112 comprise the following chemical structural formulas as shown in the figures. CVB3 resisting active research experiments show that WY92 and WY112 can inhibit cytopathic effects (CPE) generated by CVB3 on host cell Hep-2, so that survival rate of cell is enhanced, progeny virus yield is reduced, and host cell apoptosis due to CVB3 infection is inhibited. The compounds WY92 and WY112 have potential for preparing medicaments special for resisting CVB3 infection, and the compounds have the advantages of simple synthesis process, and economy and fastness; the compounds are easy for large-scale production, and have clinic application prospects.

Description

technical field [0001] The invention belongs to the technical field of antiviral drugs, and in particular relates to the application of nitrogen-containing heterocyclic aromatic ester compounds in the preparation of anti-Coxsackievirus type B3 drugs. Background technique [0002] Coxsackievirus (Coxsaekievirus) is a member of the genus Enterovirus of the family Picornaviridae, and its infection can cause a variety of diseases, such as hand, foot and mouth disease, aseptic meningitis, encephalitis, myocarditis, epidemic Myositis pain, herpetic angina, etc. There are 29 serotypes of CV reported, which can be divided into two groups, A and B, according to their pathogenic characteristics and cell sensitivity to suckling mice, namely CVA (CVA1-22, 24) and CVB ( CVB1-6). CVBs infection is the most common, among which CVB3 is the most pathogenic type among the six CVB serotypes, and is the main cause of viral myocarditis. According to the statistics of the US Centers for Diseas...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4402A61K31/4436A61P31/14
CPCA61K31/4402A61K31/4436
Inventor 魏艳红奚彩丽尧晨光李栋张谦胡康洪
Owner HUBEI UNIV OF TECH
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