Substituted calix carbazole derivative as well as synthesis method and application thereof

A technology of carbazole derivatives and derivatives, which is applied in the field of medical technology and can solve the problems of berberine hydrochloride adverse reactions and low bioavailability

Active Publication Date: 2021-11-09
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Berberine hydrochloride is a naturally occurring isoquinoline alkaloid, which has certain antibacterial effects. However, berberine hydrochloride exists in the form of flakes under physiological conditions, resulting in low bioavailability. High doses of hydrochloric acid Berberine Commonly Causes Adverse Reactions

Method used

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

Examples

Experimental program
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Effect test

Embodiment 1

[0020]

[0021] 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 A-1.

[0022]

[0023] Dissolve 3.52g of compound A-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, then remove under reduced pressure solvent, extracted with ethyl acetate, dried over anhydrous sodium sulfate, and finally purified by column chromatography to obtain compound B-1.

[0024] Dissolve 1 g of compound B-1 in dichloromethane, add paraformaldehyde (0.09 g, 3 mmol) and 0.27 g of ferric chloride, react at 27 ° C for 3-4 h, add ammonia water to quench, and then extract, The solve...

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Abstract

The invention belongs to the technical field of medicines, and relates to a substituted calix carbazole derivative as well as a synthesis method and application thereof, in particular to substituted calix [n] carbazole containing thiophene and the like as well as a synthesis method and application thereof in a drug delivery system, and in particular to application of substituted calix carbazole containing thiophene and the like in improving the drug loading function of berberine hydrochloride and reducing the cytotoxicity of drugs and application in depolymerizing protein and preparing senile dementia drugs. The chemical structural general formula of the substituted calix [n] carbazole derivative salt is shown in the specification. The substituted calix [n] carbazole derivative salt can effectively improve the cavity depth and rigid strength of calix [n] carbazole and improve the matching degree of combination of novel calix [n] carbazole and berberine hydrochloride, so as to reduce the cytotoxicity of drugs under the condition of high dosage. The calix [n] carbazole derivative can also be used for depolymerizing protein and preparing senile dementia drugs.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to substituted calixcarbazole derivatives and their synthesis methods and applications, in particular to substituted calix[n]carbazoles containing thiophene and their synthesis methods and their application in drug delivery systems, in particular to The application of calixcarbazole substituted with thiophene and the like in improving the drug-loading function of berberine hydrochloride and reducing the cytotoxicity of the drug, and the application of depolymerizing protein in the preparation of senile dementia drugs. Background technique [0002] Traditional phenol-skeleton calixarene and cyclodextrin drug carriers are limited by factors such as rigidity and cavity size, which leads to poor matching between traditional drug carriers and drug binding, and makes it difficult for drugs to be released from drug carrier cavities It is of great significance to construct a new type of drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/18C07D487/22A61P39/02A61P25/28
CPCC07D487/18C07D487/22A61P39/02A61P25/28
Inventor 杨鹏刘传峰
Owner SHENYANG PHARMA UNIVERSITY
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