A kind of 2-alkylaminoquinoline compound for preventing and treating Candida albicans and its preparation method and application

A technology of alkylamine quinoline and Candida albicans, applied in the field of biomedicine, can solve the problems of deep infection of internal tissues and organs, difficult to cure, etc.

Active Publication Date: 2020-10-23
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Under normal circumstances, Candida albicans generally does not cause disease, but when the host's immunity is low, it can cause deep infection of the body surface or even internal tissues and organs, which is usually difficult to cure

Method used

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  • A kind of 2-alkylaminoquinoline compound for preventing and treating Candida albicans and its preparation method and application
  • A kind of 2-alkylaminoquinoline compound for preventing and treating Candida albicans and its preparation method and application
  • A kind of 2-alkylaminoquinoline compound for preventing and treating Candida albicans and its preparation method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The preparation method of embodiment 1 2-alkylaminoquinoline compounds

[0028] Such as figure 1 Shown is the synthesis reaction mechanism diagram of 2-alkylaminoquinoline compounds. The specific steps of preparation are: add 0.1mmol compound A, 0.3mmol compound B, 0.04 mmol CuI, 0.15mmol KOH, 1.5mmol K 2 CO 3 , 0.02mmol BHT and 1mL dry THF were reacted at 80°C for 18h. Cool to room temperature after the reaction, extract the reaction liquid with ethyl acetate, collect the organic phase, dry with anhydrous sodium sulfate for 30 min, filter, concentrate the solvent, and separate by column chromatography to obtain the pure product.

[0029] The following are the 28 compounds obtained:

[0030]

[0031] Embodiment 2 effect detection test

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Abstract

The invention belongs to the technical field of biomedicines and in particular relates to a 2-alkylamine quinoline compound for preventing and treating candida albicans as well as a preparation methodand application of the 2-alkylamine quinoline compound. The compound is prepared from a compound A (1,2,3,4-Tetrahydroquinolines) and a compound B (O-benzoyl hydroxylamines) as raw materials throughsynthesis. Compared with the prior art, the compound has the advantages and effects that results of former research of the inventor show that a diffusible signal factor (DSF) quorum sensing signal anda derivative thereof are capable of relatively intensely interfering conversion of a yeast state to a hypha state of candida albicans, and the compound capable of inhibiting adhesion, hypha state conversion and pathogenicity of the candida albicans is successfully synthesized and screened in the research. Meanwhile, the compound is relatively small in toxicity, growth of the candida albicans andhuman cells is not affected, and the characteristics have the potential of promoting development of novel antifungal drugs.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a 2-alkylaminoquinoline compound for preventing and treating Candida albicans, a preparation method and application thereof. Background technique [0002] Candida albicans, also known as Candida albicans and Candida albicans, is an opportunistic pathogen that widely exists in nature and in the oral cavity, respiratory tract, digestive tract, and vaginal mucosa of the human body. Under normal circumstances, Candida albicans generally does not cause diseases. However, when the host's immunity is low, it can cause deep infection of the body surface or even internal tissues and organs, which is usually difficult to cure. Data show that in immunocompromised patients, the fatality rate of Candida albicans infection reaches 40%-70%. [0003] Existing studies have shown that the pathogenicity of Candida albicans is related to its yeast-hyphae two-phase transition. First...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D215/38C07D401/04A61K31/4709A61K31/5377A61K31/4725A61K31/47A61K31/496A61K31/55A61P31/10
CPCC07D215/38C07D401/04
Inventor 邓音乐张珉蒙丽丽赵赫赵朔孙秀云
Owner SOUTH CHINA AGRI UNIV
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