Novel chemical compound with anthracene ring antibiotic structure and preparation method and application thereof

A technology of antibiotics and anthracyclines, which is applied in the field of new compounds containing anthracycline antibiotics structure and its preparation and application, can solve the problems of clinical application difficulties, low solubility, application limitations, etc., and achieve the solution of application limitations and easy dissolution Effect

Inactive Publication Date: 2014-05-07
张雅珍
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Anthracycline antibiotics are currently widely used, but they often need to be turned into salts from a clinical point of view, such as doxorubicin. The common medicinal form is doxorubicin hydrochloride, which needs to be turned into hydrochloride. Its solubility is very low, it cannot be converted into salt form, so it cannot be used
After becoming hydrochloride, the pharmacodynamic function of doxorubicin is greatly reduced, so this brings great difficulties to clinical application.
[0004] Another disadvantage of anthracycline antibiotics is that due to their strong cytotoxicity, they are very toxic. They often have obvious bone marrow suppression about 10 days after use. After a week of use, they can show very obvious gastrointestinal tract Adverse reactions and cardiotoxicity, so the drug must be accurately calculated before it can be used, and the half-life of the drug is very short, which also limits the application

Method used

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  • Novel chemical compound with anthracene ring antibiotic structure and preparation method and application thereof
  • Novel chemical compound with anthracene ring antibiotic structure and preparation method and application thereof
  • Novel chemical compound with anthracene ring antibiotic structure and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] 1) The mixture of 20 g of sebacic acid in 250 ml of acetic anhydride is refluxed to form acetyl-sebacic acid;

[0043] 2) Mix 6 g of methoxypolyethylene glycol amine, 70 mg of citric acid, 200 mg of dicyclohexylcarbodiimide and 10 mg of pyridine, add 30 ml of methylene chloride, stir overnight at room temperature; then wash with ether and dry under vacuum , to obtain the polymer;

[0044] 3) Mix the products of step 1) and step 2) into a flask, and react at 150°C for 1 hour; the polymer is cooled to room temperature and dissolved in chloroform, washed with petroleum ether and dried;

[0045] 4) Put doxorubicin and step 3) 800mg of polymer into a solution mixed with 10ml of dichloromethane and 6ml of dimethyl sulfoxide; then put it in an oven for 2 hours; ultrasonically in minus 10-20 degrees 10 minutes; the product was put into 5% cholic acid solution and stirred at 600 rpm for 2 hours; it was collected by centrifugation and freeze-dried to obtain the final product.

Embodiment 2

[0047] 1. Mix 3 g of methoxypolyethylene glycol amine, 45 mg of citric acid, 260 mg of dicyclohexylcarbodiimide and 6 mg of pyridine, add 20 ml of dichloromethane, and stir overnight at room temperature;

[0048] It was then washed with ether and dried under vacuum;

[0049]2. Mix 10 g of acetyl-sebacic acid (commercially available) and the product of step 1 into a flask, and react at 120°C for 1.5 hours; the polymer is cooled to room temperature and dissolved in chloroform, washed with petroleum ether and dried to obtain a polymer 3 put pirarubicin and the polymer 1000mg into a solution mixed with 3ml methanol and 18ml dichloromethane; then put it in an oven for 14 hours; in minus 10-20 degrees, ultrasonic for 20 minutes; the product put Pour into 3% cholic acid solution and stir at 400 rpm for 4 hours; collect by centrifugation and freeze-dry to obtain the final product.

Embodiment 3

[0051] A mixture of 20 g of sebacic acid in 200 ml of acetic anhydride is refluxed to form acetyl-sebacic acid;

[0052] 2 2 g of methoxypolyethylene glycol amine, 28 mg of citric acid, 90 mg of dicyclohexylcarbodiimide and tetrahydrofuran were mixed with 15 ml of chloroform, stirred overnight at room temperature; then washed with ether and dried under vacuum to obtain a polymer ;3 Mix the products of step 1 and step 2 into a flask, and react at 150°C for 1 hour; the polymer is cooled to room temperature and dissolved in chloroform, washed with petroleum ether and dried;

[0053] 4 Put arubicin and 900mg of the polymer in step 3 into a solution mixed with 12ml of dichloromethane and 8ml of dimethyl sulfoxide; then put it in an oven for 20 hours; at minus 20-30 degrees, ultrasonic 2 minutes; the product was put into 5% cholic acid solution and stirred at 700 rpm for 2 hours; it was collected by centrifugation and freeze-dried to obtain the final product.

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Abstract

The invention discloses a novel chemical compound with an anthracene ring antibiotic structure and a preparation method and application thereof. The effect of the anthracene ring antibiotic coupling non-linear multi-block copolymer on treating choroid and retina diseases is better than that of medicines or drugs in other forms.

Description

technical field [0001] The invention discloses a new compound containing anthracycline antibiotic structure, a preparation method and application of the compound. Background technique [0002] Anthracyclines are antimitotic and extremely cytotoxic drugs. Anthracyclines can successfully inhibit a variety of malignancies, including acute leukemia, lymphoma, soft tissue and osteosarcoma, childhood malignancies, and adult solid tumors. Its mechanism of action is that the drug can penetrate into the cell and bind to the chromosome. The planar loop in the drug structure is inserted between base pairs to form a complex with DNA, which seriously interferes with DNA synthesis, DNA-dependent RNA synthesis, and protein synthesis. However, the concentration of doxorubicin required to produce an antiproliferative effect through this mechanism is higher than the concentration of the drug at the tumor site in clinical treatment. In addition, anthracycline antibiotics are also related to...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/48C07H15/252C07H1/00A61K31/704A61K31/785A61P9/10A61P27/02
Inventor 张雅珍李铁力白毅
Owner 张雅珍
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