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Applications of tetrahydroindolone/tetrahydroindazolone/tetrahydrocarbazole derivatives and salts thereof in preparation of antiviral medicine

An antiviral drug, the technology of tetrahydroindazolone, which is applied in the field of derivatives of tetrahydroindolinone/tetrahydroindazolone/tetrahydrocarbazole, can solve the problem of increasing the dose of spectral antiviral drugs, poor specificity, Poor efficacy and other issues

Active Publication Date: 2008-10-01
广州少伯控股集团有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Despite many efforts, effective drugs for the treatment of hepatitis B have not yet been developed, and therapy still relies mainly on symptomatic treatment
[0005] In clinical practice, due to the lack of targeted drugs for viral diseases, in order to inhibit the replication of viruses, the dose of spectrum antiviral drugs is often increased, which in turn leads to virus mutations, making it more difficult to effectively control
[0006] For many years, there has been a lack of effective prevention and treatment methods for diseases caused by viral infections, and traditional chemical drugs have the defects of poor specificity and poor curative effect in the treatment of viral infections.

Method used

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  • Applications of tetrahydroindolone/tetrahydroindazolone/tetrahydrocarbazole derivatives and salts thereof in preparation of antiviral medicine
  • Applications of tetrahydroindolone/tetrahydroindazolone/tetrahydrocarbazole derivatives and salts thereof in preparation of antiviral medicine
  • Applications of tetrahydroindolone/tetrahydroindazolone/tetrahydrocarbazole derivatives and salts thereof in preparation of antiviral medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Embodiment 1, anti-herpes simplex virus type 1 (HSV1) experiment

[0045] (1) Instruments and reagents: imported 96-well culture plate, inverted microscope, CO 2 Incubator, micro-sampler; culture medium is DMEM (containing 250 U / ml of green chain double antibody), adjust pH to 7.0-7.2 with sodium bicarbonate before sterilization and filtration; calf serum is inactivated at 56°C for 30 minutes Complement, sterilized and aliquoted; digestive fluid 5% trypsin + 1% EDTA + 0.01mol / L (pH7.2) PBS, sterilized and aliquoted, stored at low temperature; cell growth medium: DMEM culture medium containing 10% FBS ; Cell maintenance fluid: DMEM culture fluid containing 1% FBS; Positive drug: acyclovir ACV; Test drug: tetrahydroindolinone / tetrahydroindazolone / tetrahydrocarbazole derivatives as described in Table 1 (Structural formulas I-01 to I-55).

[0046] (2) Virus and cell strain: herpes simplex virus type I virus strain HSV-1 (ATCC, VR733, F strain), through Vero cell subcultur...

Embodiment 2

[0072] Embodiment 2, anti-herpes simplex virus type II (HSV2)

[0073] (1) Instruments and reagents: refer to Example 1.

[0074] (2) Virus and cell strain: herpes simplex virus type II virus strain HSV-2 (provided by Wuhan Typical Species Preservation Center), and the titration of Vero cells is about 10 5 TCID 50 ; Cell line: African green monkey kidney cells (Vero), derived from American ATCC, CCL81 strain.

[0075] (3) Drug treatment: refer to Example 1.

[0076] (4) Measuring method: refer to Example 1.

[0077] (5) Cytotoxicity test of drugs: refer to Example 1.

[0078] (6) Antiviral activity test of medicine: refer to Example 1.

[0079] (7) Experimental results

[0080] 1) Cytotoxic MTT assay results:

[0081] The compounds of tetrahydroindolinone derivatives and tetrahydroindolinone derivatives all showed lower cytotoxicity to Vero cells, and their TC 50 See Table 2.

[0082] The maximum non-toxic concentration of each sample was selected as the maximum drug ...

Embodiment 3

[0088] Embodiment 3, anti-Coxsackie virus experiment

[0089] (1) Instruments and reagents: imported 96-well culture plate, inverted microscope, CO 2 Incubator, micro-sampler; culture medium is DMEM (containing 250 U / ml of green chain double antibody), adjust pH to 7.0-7.2 with sodium bicarbonate before sterilization and filtration; calf serum is inactivated at 56°C for 30 minutes Complement, sterilized and aliquoted; digestive fluid 5% trypsin + 1% EDTA + 0.01mol / L (pH7.2) PBS, sterilized and aliquoted, stored at low temperature; cell growth medium: DMEM culture medium containing 10% FCS Cell maintenance fluid: DMEM culture fluid containing 1%FCS; Positive drug: ribavirin; Test drug: the compound described in Table 1 of Tetrahydroindole derivatives and Tetrahydroindazole derivatives (structural formula sees I- in Table 1 01 to I-55).

[0090] (2) Cells and virus strains Cells: cervical cancer cells (Hela), derived from ATCC in the United States, CCL81 strain virus: CVB3 (pr...

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Abstract

The invention relates to an application of tetrahydroindolone / tetrahydroindazolone / tetrahydrocarbazole derivatives and salts thereof in the preparation of antiviral drugs. The tetrahydroindolone derivatives, the tetrahydroindazolone derivatives or the tetrahydrocarbazole derivatives, as well as the salts thereof of the invention have anti-viral functions, and the virus comprises I-typed and II-typed herpes virus, coxsackie virus type 3 (CVB3) and hepatitis B virus.

Description

technical field [0001] The invention relates to the application of derivatives of tetrahydroindolinone / tetrahydroindazolone / tetrahydrocarbazole and salts thereof in the preparation of antiviral drugs. Background technique [0002] In view of the global prevalence of viral diseases such as SARS, bird flu, and mad cow disease in recent years, the development of antiviral drugs has become a hot spot of widespread concern. At present, the main strategies of antiviral drug research in the world include: blocking the combination of virus and target cells, inhibiting reverse transcriptase, inhibiting viral protein translation, inhibiting protein modification or budding of virus particles, and cutting off the viral genome. Through structural modification of known therapeutic compounds, computer design of lead molecules, structural modification of antisense oligonucleotides and combinatorial chemical synthesis, development of immune function modulators, and screening of natural antiv...

Claims

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Application Information

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IPC IPC(8): A61K31/4439A61K31/497A61K31/404A61K31/403A61K31/5377A61K31/416A61K31/4155A61P31/12
Inventor 王一飞夏敏邢国文
Owner 广州少伯控股集团有限公司
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