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Application of dehydrocamelinarum derivatives as preparation of medicaments for the treatment of cystic hydatid disease

A technology of dehydrohaeline and cystic echinococcosis, applied in the direction of drug combination, pharmaceutical formula, anti-infective drugs, etc., can solve the problems of reducing the survival rate of Echinococcus granulosus and high toxicity

Active Publication Date: 2020-06-09
THE FIRST TEACHING HOSPITAL OF XINJIANG MEDICAL UNIVERCITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The present invention provides a dehydrohaeline derivative used as a drug for treating cystic echinococcosis, which overcomes the above-mentioned deficiencies in the prior art, and can effectively solve the problem of treating cystic echinococcosis with dehydrohaeline monomer. The toxicity of the disease exists; the present invention discloses for the first time the application of dehydrohalamine derivatives as a drug for the preparation of cystic echinococcosis; the in vitro pharmacodynamic experiment data show that dehydrohalamine derivatives can significantly reduce The survival rate of Echinococcus granulosus; the in vivo pharmacodynamic experimental data show that dehydrohaeline derivatives are equivalent to albendazole in the treatment of cystic echinococcosis; the in vivo and in vitro safety evaluation experimental data show that dehydrocameline derivatives The toxicity of sacarpine derivatives is less than that of dehydrohalamine monomer with anti-cystic echinococcosis activity, thus providing a new way for the treatment of cystic echinococcosis

Method used

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  • Application of dehydrocamelinarum derivatives as preparation of medicaments for the treatment of cystic hydatid disease
  • Application of dehydrocamelinarum derivatives as preparation of medicaments for the treatment of cystic hydatid disease
  • Application of dehydrocamelinarum derivatives as preparation of medicaments for the treatment of cystic hydatid disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Embodiment 1: the structural general formula of dehydrohaemaline derivative is:

[0065]

[0066] Among them, R1 is selected from hydrogen, C1-4 alkyl, substituted or unsubstituted five-membered aryl or six-membered aryl, substituted or unsubstituted containing 1 to 4 heteroatoms selected from N or O or S One of five-membered heteroaryl or six-membered heteroaryl, R9 is one selected from hydrogen, C1-6 alkyl, hydroxy-C1-6 alkyl, aryl-C1-6 alkyl.

Embodiment 2

[0067] Example 2: As an optimization of the above examples, the substituents on the substituted or unsubstituted five-membered aryl or six-membered aryl are selected from hydroxyl, amino, carboxyl, halogen, nitro, C1-6 alkyl and C1- One of 6 alkoxy groups.

Embodiment 3

[0068] Embodiment 3: As the optimization of the above-mentioned embodiment, the dehydrohaemaline derivative is 1-(4-methoxy)phenyl-9-butyl-β-carboline, and its structural formula is:

[0069]

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Abstract

The invention relates to the technical field of application of a harmine derivative, and particularly discloses the application of a harmine derivative to preparation of drugs for treating cystic echinococcosis for the first time. In-vitro pharmacodynamic experiment data prove that the harmine derivative can reduce the survival rate of echinococcosis granulosis cyst remarkably; In-vivo pharmacodynamic experiment data prove that the efficacy of the harmine derivative and the efficacy of albendazole are similar in treating cystic echinococcosis; in-vitro-and-vivo safety evaluation experiment data prove that the toxicity of the harmine derivative is lower than that of a harmine monomer with cystic echinococcosis resisting activity. Therefore, a new approach is provided for treating cystic echinococcosis.

Description

technical field [0001] The invention relates to the application technical field of dehydrohaeline derivatives, and relates to the application of a dehydrohaeline derivative as a medicine for treating cystic echinococcosis. Background technique [0002] Hydatid disease, also known as echinococcosis, is a serious zoonotic parasitic disease caused by the parasitic larvae of Echinococcus tapeworm in the human body, and 95% of the cases are larval cysts of Echinococcus granulosus Cystic echinococcosis in humans. The disease is distributed globally. Seven provinces (autonomous regions) including Xinjiang, Tibet, Ningxia, Qinghai, Gansu, Inner Mongolia, and Sichuan in western my country are high-incidence areas, causing economic losses of more than 3 billion yuan every year. It is one of the main causes of poverty and return to poverty due to illness, and it is also a serious public health problem that has attracted much attention. In 2006, the disease was included in the national ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/437A61P33/10C07D471/04
CPCA61K31/437
Inventor 温浩武嘉林王建华许兆辉赵军马芹马运芳周凡陈蓓郭亮高惠静范文玺吕国栋
Owner THE FIRST TEACHING HOSPITAL OF XINJIANG MEDICAL UNIVERCITY
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