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Dendritic tryptophan compound, preparation method thereof and application of dendritic tryptophan compound as virus invasion inhibitor

A compound, tryptophan technology, applied in the direction of antiviral agents, etc., can solve the problem of weakening the curative effect, achieve a wide range of antiviral properties, short reaction cycle, and meet the effects of industrialized large-scale production

Active Publication Date: 2020-08-11
WEIHAI CY DENDRIMER TECH
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  • Abstract
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Problems solved by technology

However, this approach suffers from long-term side effects, latent viral infection, and the development of drug resistance, thereby undermining the efficacy of all clinically available drugs

Method used

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preparation example Construction

[0027] The present invention proposes a kind of preparation method of dendritic tryptophan compound, comprises the following steps:

[0028] Add carboxy-terminated polyamide-amine dendrimers and alkyl-esterified tryptophan to hydrochloric acid and N,N-dimethylformamide solution, and react at 20°C-60°C for 3-10 days to obtain terminally colored Compounds with amino acid groups;

[0029] Carrying out rotary evaporation drying, washing, and drying the above-mentioned compound containing a tryptophan group at the end, and purifying the obtained residue by high performance liquid chromatography to obtain a preliminary purified compound containing a tryptophan group at the end;

[0030] Dissolve the initially purified compound containing a tryptophan group in THF solution, add LiOH aqueous solution, stir at 20°C-60°C for 3-10 days, add formic acid to adjust the pH to 2, and dry it by rotary evaporation The residue was purified by high performance liquid chromatography to obtain the...

Embodiment 1

[0046] Dissolve 0.1mol of the first-generation PAMAM and 0.4mol of succinic anhydride in 100ml of dimethyl sulfoxide (DMSO), respectively, add the DMSO solution of PAMAM to the DMSO solution dissolved in succinic anhydride, and react at 40°C 2 days; the reaction solution was added dropwise to 10 times the volume of acetone to precipitate, and then washed 3 times with acetone, dissolved in deionized water, dialyzed for 2 days and freeze-dried to obtain the carboxyl-terminated dendritic polymer 1, and the yield was 93%.

Embodiment 2

[0048] Dissolve 0.1mol second-generation PAMAM and 1.6mol succinic anhydride in 100ml DMSO respectively, add the DMSO solution of PAMAM to the DMSO solution dissolved in succinic anhydride, and react at 40°C for 3 days; Add to 10 times volume of acetone for precipitation, wash with acetone for 3 times, dissolve in deionized water, dialyze for 2 days and freeze-dry to obtain carboxyl-terminated dendritic polymer 2 with a yield of 94%.

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Abstract

The invention discloses a dendritic tryptophan compound, a preparation method of the dendritic tryptophan compound and application of the dendritic tryptophan compound serving as a virus invasion inhibitor, and belongs to the technical field of dendritic polymer synthesis. According to the technical scheme, the preparation method comprises the following steps: adding a carboxyl-terminated polyamide-amine dendritic compound and alkyl esterified tryptophan into a hydrochloric acid and N, N-dimethylformamide solution, and reacting at 20-60 DEG C for 3-10 days to obtain a compound containing tryptophan groups at the tail end; and carrying out rotary evaporation drying, washing and drying on the compound containing the tryptophan group at the tail end, and carrying out high performance liquid chromatography purification on an obtained residue to obtain a preliminarily purified compound containing the tryptophan group at the tail end. The compound is applied to the aspect of virus invasion inhibitors, can solve the problems of the existing virus invasion inhibitors, and has the characteristics of simple preparation method, good antiviral effect and wide antiviral property.

Description

technical field [0001] The invention belongs to the technical field of dendritic polymer synthesis, and in particular relates to a dendritic tryptophan compound, its preparation method and its application as a virus invasion inhibitor. Background technique [0002] Devastating infectious diseases such as the human immunodeficiency virus (HIV) are one of the major global public health problems. Currently, the most commonly used approach is antiretroviral therapy, which can improve and change the viral infection into a manageable chronic disease. However, this approach suffers from long-term side effects, latent viral infection, and the development of drug resistance, thereby undermining the efficacy of all clinically available drugs. Therefore, new inhibitors and antiviral therapeutic strategies are urgently needed. [0003] Studies have shown that compounds containing tryptophan (Trp) groups are essential groups for their antiviral activity against HIV and EV71 viruses due...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G73/02A61P31/12A61P31/18
CPCC08G73/028A61P31/12A61P31/18
Inventor 李武松刘聪聪
Owner WEIHAI CY DENDRIMER TECH
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