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Small-molecule inhibitor of influenza virus

An influenza virus and inhibitor technology, applied in the field of influenza virus small molecule inhibitors, can solve the problem of easy mutation and drug resistance of influenza virus and other problems

Active Publication Date: 2021-11-23
INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the mutating nature of influenza viruses makes drug resistance a growing problem

Method used

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  • Small-molecule inhibitor of influenza virus
  • Small-molecule inhibitor of influenza virus
  • Small-molecule inhibitor of influenza virus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1, the inhibitory efficacy evaluation of pralatrexate

[0029] 1. Evaluation of the inhibitory effect of pralatrexate on H1N1 influenza virus by multi-concentration gradient experiments at the cell level

[0030] 1. Add dual antibodies (penicillin and streptomycin) and TPCK (final concentration: 2 μg / ml) to the DMEM medium to prepare a maintenance solution, and use this maintenance solution to dilute the influenza virus so that the titer of the influenza virus is 100 TCID 50 / 25μl maintenance solution.

[0031] 2. Dissolve pralatrexate with 100% DMSO and prepare a 40mM mother solution, then use the maintenance solution prepared in step 1 to dilute the mother solution 5 times in a gradient to different concentrations (100 μM, 20 μM, 4 μM, 0.8 μM, 0.16 μM, 0.032μM, 0.0064μM, 0.00128μM, 0.000256μM, 0.0000512μM) solutions to be tested, each concentration volume is 50ul. The final concentration of DMSO in the test solution was 0.02% (volume percentage), and a ne...

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Abstract

The invention discloses a small-molecule inhibitor of influenza virus. The small-molecule inhibitor is pralatrexate, the structural formula of the pralatrexate is shown as a formula I, and the small-molecule inhibitor can inhibit influenza viruses, specifically influenza A viruses such as H1N1, H5N1 or H5N6 subtype influenza viruses. The research finds that the small-molecule inhibitor has a remarkable inhibition effect on H1N1, H5N6 and H5N1 subtype influenza viruses, and the compound shown in the formula I has broad-spectrum anti-influenza A virus potential preliminarily; meanwhile, the toxicity of the small-molecule inhibitor to cells is small, the CC50 of the small-molecule inhibitor to MDCK cells is larger than 200 mu M, the CC50 / EC50 ratio (namely the selectivity index SI) is larger than 200, and the small-molecule inhibitor can be used as a safe and effective anti-influenza virus medicine.

Description

technical field [0001] The invention relates to a small molecule inhibitor of influenza virus, which belongs to the technical field of medicinal chemistry. Background technique [0002] Influenza viruses belong to the Orthomyxoviridae family and can cause acute respiratory infectious diseases. According to the antigenicity of nucleoprotein and matrix protein, influenza virus can be divided into four types: A, B, C, and D. Among them, influenza A virus can infect various animals including humans, poultry, pigs, horses, etc. In addition to the H1 / H2 / H3 subtype influenza viruses that can cause seasonal influenza or influenza pandemics, various subtypes (H5, H6, H7, H9, H10) influenza viruses have infected human cases, endangering human life and health. posed a huge threat. [0003] The World Health Organization estimates that seasonal influenza viruses cause as many as 650,000 deaths and 3 to 5 million severe infections worldwide each year. The World Health Organization rec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61P31/16A61P1/00
CPCA61K31/519A61P31/16A61P11/00
Inventor 施一王敏杨薇苏佳岐彭如超彭齐
Owner INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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