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Substituted calix [4] carbazole derivative as well as synthesis method and application thereof

A technology of carbazole derivatives and azole derivatives, applied in the field of medicine, can solve the problems of poor biocompatibility of drug carriers, low matching degree of drug carriers, and high toxicity of drug carriers

Active Publication Date: 2022-05-13
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Traditional phenol-skeleton calixarene and cyclodextrin drug carriers are limited by factors such as poor biocompatibility, cavity size, high self-toxicity and poor fluorescence performance, resulting in a poor match between traditional drug carriers and drugs , The poor biocompatibility of drug carriers is not conducive to entering cells. At the same time, many drug carriers have high toxicity and are difficult to use as drug carriers. Poor autofluorescence is not conducive to cell positioning. Therefore, new drug carrier macromolecules are constructed and applied It is of great significance in drug delivery, heavy metal ion removal and cell localization

Method used

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  • Substituted calix [4] carbazole derivative as well as synthesis method and application thereof
  • Substituted calix [4] carbazole derivative as well as synthesis method and application thereof
  • Substituted calix [4] carbazole derivative as well as synthesis method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Preparation method one:

[0038]

[0039] Dissolve 2.06g of 5-bromothiophene-2carboxylic acid in sulfur oxychloride, reflux for 5h, remove the solvent under reduced pressure, add toluene solution, 1.8g of triethylene glycol monomethyl ether and pyridine, reflux for 6h, then remove under reduced pressure solvent, extracted with ethyl acetate, dried over anhydrous sodium sulfate, and finally purified by column chromatography to obtain compound 1.

[0040]

[0041] Dissolve 3.52g of compound 1 and 2.7g of 2,7-dimethoxy-9H-carbazole in DMF, then add cuprous iodide and potassium carbonate, react at 130°C for 3h, and then remove the solvent under reduced pressure , extracted with ethyl acetate, dried over anhydrous sodium sulfate, and finally purified by column chromatography to obtain compound 2.

[0042]

[0043] Dissolve 1 g of compound 2 in dichloromethane, add paraformaldehyde (3 mmol) and 0.27 g of ferric chloride, react at 27 ° C for 3-4 h, add ammonia to que...

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Abstract

The invention belongs to the technical field of medicines, and relates to a substituted calix [4] carbazole derivative as well as a synthesis method and application thereof, in particular to substituted calix [4] carbazole containing thiophene, acylhydrazone bonds, gallic acid and the like, a synthesis method of the substituted calix [4] carbazole, and application of the substituted calix [4] carbazole in a drug delivery system, recognition of heavy metal ions, Abeta40 (beta-amyloid protein) entrapment and cell localization. The invention relates to a substituted calix [4] carbazole derivative of which the chemical structural general formula is shown in the specification. According to the substituted calix [4] carbazole derivative, the matching degree of combination of calix [4] carbazole and adriamycin can be improved, and the bioavailability of adriamycin is effectively improved; the combination with mercury ions is improved, and the mercury ions in the blood can be cleared; the calix [4] carbazole can entrap A [beta] 40 protein, can effectively remove A [beta] 40 and is beneficial to treatment of senile dementia, and calix [4] carbazole has good fluorescence performance and is beneficial to observation and localization at a cell position.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a substituted calix[4]carbazole derivative and a synthesis method and application thereof, in particular to a substituted calix[4]carbazole containing thiophene, an acylhydrazone bond, and gallic acid, and a synthesis method thereof. Its applications in drug delivery systems, recognition of heavy metal ions, Aβ40 (β-amyloid) entrapment and cell localization. Background technique [0002] Doxorubicin is currently mainly used for acute leukemia, malignant lymphoma and breast cancer, etc., but its bioavailability is poor. By using the hydrophobic cavity of the drug carrier, doxorubicin is entrapped to form drug nanoparticles and transported into the body to improve its bioavailability. Use, and then improve the effect of treating tumors. [0003] Alzheimer's disease is related to the aggregation of Aβ40 (β-amyloid) protein, and the hydrophobic cavity of the carrier is used to transp...

Claims

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Application Information

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IPC IPC(8): C07D487/22A61K31/704A61P35/00C09K11/06A61K47/22G01N21/64
CPCC07D487/22A61K31/704A61P35/00C09K11/06A61K47/22G01N21/6486C09K2211/1074C09K2211/1092
Inventor 杨鹏刘传峰
Owner SHENYANG PHARMA UNIVERSITY
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