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A kind of antiviral drug molecule that inhibits influenza virus rna polymerase activity and preparation method thereof

A technology of RNA polymerase and drug molecules, applied in antiviral agents, organic active ingredients, pharmaceutical formulations, etc., can solve the problems of limited influenza virus drugs and obvious side effects

Active Publication Date: 2021-01-08
HKUST SHENZHEN RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide an antiviral drug that inhibits the activity of influenza virus RNA polymerase and its preparation method, aiming to solve the problems of limited and obvious side effects of existing influenza virus drugs

Method used

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  • A kind of antiviral drug molecule that inhibits influenza virus rna polymerase activity and preparation method thereof
  • A kind of antiviral drug molecule that inhibits influenza virus rna polymerase activity and preparation method thereof
  • A kind of antiviral drug molecule that inhibits influenza virus rna polymerase activity and preparation method thereof

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preparation example Construction

[0033] Correspondingly, the embodiment of the present invention provides a preparation method of an antiviral drug molecule that inhibits the activity of influenza virus RNA polymerase, the structure of the drug molecule is shown in the following formula 1, and the preparation method includes the following steps:

[0034] S01. Provide tetrahydroisoquinoline substrate shown in formula 2, benzaldehyde and trimethylsilyl acetylene shown in formula 3, add benzoic acid and cuprous iodide, and react at 75°C-85°C for 10-13 Hour, filter and concentrate to obtain crude product; Crude product is dissolved in the alcoholic solvent, adds potassium carbonate or sodium carbonate, reaction knot preparation tetrahydroisoquinoline shown in formula 4;

[0035] S02. Take tetrahydroisoquinoline shown in formula 4, add HCO 2 Na and palladium catalysts, a ring-closing reaction occurs under an inert atmosphere at a temperature of 95-105 ° C, and the compound shown in formula 5 is prepared;

[0036]...

Embodiment 1

[0054] A preparation method of an antiviral drug molecule that inhibits the activity of influenza virus RNA polymerase, the structure of the drug molecule is shown in formula 1, and the preparation method comprises the following steps:

[0055] Provide 212 mg of tetrahydroisoquinoline shown in formula 2, 229 mg of benzaldehyde shown in formula 3 and 0.26 mL of trimethylsilyl acetylene, add 12 mg of benzoic acid, 19 mg of CuI, react at 80 ° C for 12 hours, filter and concentrate to obtain a crude product, and The crude product was dissolved in 10ml of methanol, 276mg of potassium carbonate was added, and after the reaction was completed, 297mg of tetrahydroisoquinoline represented by formula 4 was obtained by column chromatography;

[0056] Get tetrahydroisoquinoline 215mg shown in formula 4 and place in the flask, add DMF (9mL), H 2 O (3mL), then add HCO 2 Na (68 mg), saturated with nitrogen for 15 minutes, then added Pd (PPh 3 ) 4 (29 mg), placed in an oil bath at 100°C fo...

Embodiment 2

[0061] Cell culture and transfection of HEK-293T

[0062] For the in vitro screening of anti-influenza virus drugs, the embodiment of the present invention selects a cell culture model. Specifically, the embodiment of the present invention selects HEK-293T cells. This model can effectively eliminate the influence of other external factors, and only study the influence of the drug molecule of the embodiment of the present invention on the influenza virus RNA polymerase, so as to provide more basis for later mechanism research. The cell model can be used to screen the direct inhibitory effect of the drug molecule on the influenza virus, and quantitatively analyze the effect of the drug molecule of the present invention on the cytotoxicity and the activity of the influenza virus.

[0063] Prepare the required culture medium and solution: prepare TransIT-1L transfection agent, specifically, the composition of the medium is 5% FBS and 1% P / S Opti-MEM medium, which can effectively ...

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Abstract

The invention provides an antiviral pharmaceutical molecule capable of inhibiting the activity of influenza virus RNA polymerase. An antiviral drug contains the structure represented by the followingformula 1, or the antiviral drug contains a compound with the structure represented by the formula 1 as a drug precursor.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to an antiviral drug molecule for inhibiting the activity of influenza virus RNA polymerase and a preparation method thereof. Background technique [0002] Influenza viruses are referred to as influenza viruses for short, and currently mainly include three types, influenza A virus, influenza B virus and influenza C virus. Influenza A virus can infect humans and many kinds of animals. It has strong infectivity and transmissibility, and can easily cause seasonal influenza pandemics. Humans can become infected with avian or other zoonotic influenza viruses through contact with infected animals or a contaminated environment. Such as A H5N1, H7N9, H9N2 and other avian influenza viruses. Human infection with influenza virus can cause severe pneumonia, sepsis accompanied by shock, etc., and even death, which seriously affects the national economy and human health. For exam...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4745A61P31/16
CPCA61K31/4745A61P31/16
Inventor 黄旭辉张柏恒童荣标许新洲谢良旭周世强
Owner HKUST SHENZHEN RES INST
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