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Anti-RNA (Ribonucleic Acid) virus drug quinoline derivative and application thereof

A RNA virus and drug technology, applied in the field of treatment of viral infections, can solve the problems of high research and development costs, emergence of drug resistance, and long time

Pending Publication Date: 2021-10-01
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this antiviral drug can achieve high specificity and selectivity, long-term and large-scale use often leads to drug resistance, and the cost of research and development is high and time-consuming, lacking predictability

Method used

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  • Anti-RNA (Ribonucleic Acid) virus drug quinoline derivative and application thereof
  • Anti-RNA (Ribonucleic Acid) virus drug quinoline derivative and application thereof
  • Anti-RNA (Ribonucleic Acid) virus drug quinoline derivative and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0093] Embodiment 1. The inhibitory activity and cytotoxicity evaluation of the compound of the present invention to 2019 new coronavirus (2019-nCoV), Ebola virus, avian influenza virus A / GuangZhou / 99 (H9N2)

[0094] Materials and methods: Buquina is commercially available with a purity of over 98%, and the series of Buquina derivatives were purchased from Compound Library.

[0095] Detection methods and results:

[0096] 1. Anti-2019 novel coronavirus (2019-nCoV) drug efficacy experiment detected by fluorescent quantitative PCR method:

[0097] References (Wu Zhong, et al. Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitro, Cell Research (2020), 1–3, Zhou, P., et al. A pneumonia outbreak associated with a new coronavirus of probable bat origin.Nature 2020) method, infected with 2019BetaCoV / Wuhan / WIV04 / 2019 strain) infection amount MOI=0.03 on Vero E6 cells (ATCC-1586), and added different dilutions of drugs at the same ...

Embodiment 2

[0118] Embodiment 2, the antiviral activity evaluation of the combination of the compound of the present invention and other antiviral drugs

[0119] The inventor further tested Buquina and other antiviral drugs of the prior art, including lopinavir, ritonavir, ribavirin, remdesivir, oseltamivir, Tamiflu, Lani Combination of one or more of Mivir, Peramivir and Chloroquine (Chloroquine Phosphate).

[0120] It was found that the combination of buquina and these antiviral drugs can produce better therapeutic effect; among them, the combination of lopinavir, ritonavir, ribavirin, remdesivir and chloroquine (chloroquine phosphate) The treatment effect is relatively good.

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Abstract

The invention discloses a compound shown in a formula I or the application of pharmaceutically acceptable salt thereof in drugs for treating RNA virus infection. The drugs have broad-spectrum and excellent anti-RNA virus activity, and have low toxicity to normal cells.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry; specifically, the present invention relates to the preparation of buquina to treat RNA virus infection and its application in the treatment of viral infection. Background technique [0002] Diseases caused by acute viral infections are an important threat to public health security. These viruses include not only well-known influenza viruses, but also some emerging new viruses such as coronaviruses. [0003] Diseases caused by virus infection are an important threat to public health security. These viruses include not only the well-known influenza virus, Ebola virus, bunya virus, avian influenza virus H9N2, H1N1, H7N9, arenavirus, rabies virus, HCV, HBV, HIV-1, HSV-1, HSV-2, etc., also including coronaviruses such as severe acute respiratory syndrome coronavirus (SARS-CoV), Middle East respiratory syndrome coronavirus (MERS-CoV) and 2019 novel coronavirus ( 2019-nCoV). [0004] Coronav...

Claims

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Application Information

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IPC IPC(8): A61K31/47A61K31/4709A61K45/06A61P31/14A61P31/20A61P31/18A61P31/16A61P31/22A61K31/513A61K31/7056A61K31/4706A61K31/427
CPCA61K31/47A61K31/4709A61K45/06A61P31/14A61P31/20A61P31/18A61P31/16A61P31/22A61K31/513A61K31/7056A61K31/4706A61K31/427A61K2300/00
Inventor 李洪林刁妍妍赵振江李诗良朱丽丽
Owner EAST CHINA UNIV OF SCI & TECH
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