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Application of heterocyclic compound in preparation of medicine for treating pneumonia

A technology of heterocyclic compounds and pneumonia, which is applied in the application field of heterocyclic compounds in the preparation of drugs for the treatment of pneumonia, can solve the problems of mycoplasma pneumonia patients increase, pneumonia recurrence, azithromycin resistance, etc., and achieve excellent anti-pneumonia activity Effect

Active Publication Date: 2020-07-03
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, azithromycin, a classic drug clinically used to treat Mycoplasma pneumoniae, has developed drug resistance, leading to recurrence of pneumonia after treatment, and the number of patients with refractory Mycoplasma pneumonia is increasing year by year

Method used

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  • Application of heterocyclic compound in preparation of medicine for treating pneumonia
  • Application of heterocyclic compound in preparation of medicine for treating pneumonia
  • Application of heterocyclic compound in preparation of medicine for treating pneumonia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] This example describes the preparation methods of compound 1 to compound 24 in detail.

[0028] According to a preferred embodiment, compounds 1 to 24 are through cyclization reaction, acidification reaction, ethylation reaction, addition reaction, substitution reaction, catalytic reaction, nitrosation reaction, reduction reaction, formylation reaction, and methylation reaction. In one or more reactions.

[0029] This example provides the preparation methods of 24 kinds of heterocyclic compounds. All the prepared heterocyclic compounds have their structures determined by infrared spectroscopy (IR), nuclear magnetic resonance spectroscopy (NMR) and mass spectrometry.

[0030] Preparation of compound 1

[0031] Compound 1 has the following structure:

[0032]

[0033] The preparation process of compound 1 is as follows, and the main starting materials for each reaction step below are calculated as 1 mmol.

[0034] ①1mmol of CNCH 2 COCH 3 (CH 2 CH 3 )CONH 2 The derivative was cycliz...

Embodiment 2

[0121] In this example, the activity of compounds 1-24 prepared in Example 1 against pneumonia caused by Streptococcus pneumoniae was tested.

[0122] Experimental method: Pneumonia model caused by Streptococcus pneumoniae in vivo: SPF male SD male rats (weight about 200g) were randomly divided into several groups, including blank control group, model group, positive control group of cefuroxime axetil tablets, and the like Caffeine group, caffeine analog group (the substances used in the caffeine analog group are: 1-propyl 3,7-dimethylxanthine (caffeine analog A), 1-isopropyl 3,7- Dimethylxanthine (caffeine analog B), 3-ethyl 3,7-dimethylxanthine (caffeine analog C)) and compound 1 to 24 groups, 8 in each group, under standard environment Raised for 7 days. Before the experiment, the rats were lightly anesthetized with ether, and then by nasal inhalation, in addition to the nasal instillation of normal saline in the blank control group, the model group, the positive control grou...

Embodiment 3

[0128] In this example, the activity of compounds 1-24 prepared in Example 1 against influenza A virus pneumonia was tested.

[0129] C57 mice (22-25g) were randomly divided into several groups, namely the blank control group (Normal), model group (Model), oseltamivir positive control group, analog caffeine group, and caffeine analog group ( The substances used in the caffeine analog group are: 1-propyl 3,7-dimethylxanthine (caffeine analog A), 1-isopropyl 3,7-dimethylxanthine (caffeine analog B), 3-ethyl 3,7-dimethylxanthine (caffeine analog C)), compound 1-24 group. On the first day, the mice were inoculated with influenza A virus. Except for mice in the blank control group who were instilled with normal saline through the nose, the mice in all other groups were infected with influenza A H1N1 strain FM1 (30 μL) through the nose. After 24 hours, the mice in the blank control group and the model group were given the same dose of normal saline in the drug group, and the mice in t...

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Abstract

The invention discloses an application of heterocyclic compounds in preparation of medicines for treating pneumonia, and relates to the technical field of biomedicine. According to the application ofthe heterocyclic compounds in the preparation of the medicines for treating the pneumonia provided by the invention, the heterocyclic compounds have anti-pneumonia activity, wherein the pneumonia includes but is not limited to viral pneumonia, bacterial pneumonia, mycoplasma pneumonia, and chlamydia pneumonia. The anti-pneumonia pharmacological activity of the structurally modified and transformedheterocyclic compounds is tested, the pharmacological activity of the compounds is tested in multiple pneumonia models, and data of anti-pneumonia activity are provided to confirm that the heterocyclic compounds all have excellent anti-pneumonia activity, that is, the heterocyclic compounds with antipneumonia activity are screened out, so that a novel skeleton can be provided for screening a novel compound for treating the pneumonia, and a theoretical foundation is laid for development of a novel lead compounds.

Description

Technical field [0001] The invention relates to the technical field of biomedicine, in particular to the application of a heterocyclic compound in the preparation of a medicine for treating pneumonia. Background technique [0002] Pneumonia is a disease of the respiratory system, but if this inflammation is not well controlled, it can cause various complications. First of all, pneumonia can cause lung damage, which can damage the alveolar respiratory tract mucosa. If the inflammation is not well controlled, it can also cause respiratory failure and septic shock. When viruses or bacteria spread into the blood circulation, they can also cause sepsis. When inflammatory factors enter the heart through the blood circulation, it can also cause myocarditis and even cause sudden death from heart failure. [0003] Viral pneumonia is an upper respiratory tract infection caused by a virus, and it spreads to the lungs to cause inflammation. It is accompanied by systemic fever, soreness, hea...

Claims

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Application Information

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IPC IPC(8): A61K31/437A61K31/519A61K31/517A61K31/473A61K31/435A61K31/122A61K31/522A61K31/513A61K31/52A61P11/00A61P31/12A61P31/04A61P31/10A61P37/02A61P31/16A61P31/14
CPCA61K31/122A61K31/435A61K31/437A61K31/473A61K31/513A61K31/517A61K31/519A61K31/52A61K31/522A61P11/00A61P31/04A61P31/10A61P31/12A61P31/14A61P31/16A61P37/02
Inventor 黄文
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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