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Anti-candida albicans piperazine derivative, preparation method therefor and application thereof

A technology of Candida albicans and its derivatives, which is applied in the direction of antifungal agents, medical preparations containing active ingredients, pharmaceutical formulas, etc., to achieve a high yield effect

Active Publication Date: 2019-03-19
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the most effective treatment and prevention of Candida albicans infection is local and systemic use of azole antifungal drugs, which can directly kill bacteria, but with the widespread use of azole drugs, drug resistance is becoming more and more serious

Method used

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  • Anti-candida albicans piperazine derivative, preparation method therefor and application thereof
  • Anti-candida albicans piperazine derivative, preparation method therefor and application thereof
  • Anti-candida albicans piperazine derivative, preparation method therefor and application thereof

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Embodiment 1

[0038] The synthesis of embodiment 1 piperazine derivatives

[0039] One, such as figure 1 Shown, the synthetic process of piperazine derivatives is as follows:

[0040] (1) First, mix 4-hydroxyindole, 4-hydroxycarbazole or 4-hydroxyacetophenone with epichlorohydrin (molar ratio is 1:1.2), and drop the mass (g) volume ( mL) ratio of 40% sodium hydroxide aqueous solution (the amount of NaOH is 2 times of the molar number of 4-oxindole, 4-hydroxycarbazole or 4-hydroxyacetophenone), after the dropwise addition is completed, the temperature is raised to 60°C, and the reaction , to obtain the corresponding epoxy compound, TLC (thin layer chromatography, material is silica gel GF254) detection reaction process, until the raw material point disappears, developing agent is sherwood oil: the mixed solution that ethyl acetate obtains by volume ratio 7: 1, and reaction finishes Then add water, extract with ethyl acetate, combine the organic phases, wash with water, dry with anhydrous m...

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Abstract

The present invention provides an anti-Candida albicans piperazine derivative, a preparation method therefor and application thereof. The structural formula of the piperazine derivative is as represented by formula I. The piperazine derivative has the advantages of that the piperazine derivative is a compound capable of inhibiting Candida albicans adhesion, hyphal morphology conversion and pathogenicity, and at the same time, the compound has low toxicity and does nto influence growth of Candida albicans and cells of humans. Therefore, the piperazine derivative is expected to be developed intoa new anti-Candida albicans infection drug.

Description

technical field [0001] The invention relates to the field of compound synthesis, in particular to a piperazine derivative against Candida albicans and its preparation method and application. Background technique [0002] Candida albicans is a fungal disease widely spread in humans, and it is one of the most important pathogens of hospital-acquired infection. The fungus infects and colonizes a wide range of microbial environments in the human body, including blood vessels, mucosal surfaces and major internal organs. As an opportunistic pathogen, Candida albicans is not only the pathogen of oral thrush and vaginitis, but also can cause severe systemic infection and high mortality in immunocompromised patients. At present, the most effective treatment and prevention of Candida albicans infection is local and systemic use of azole antifungal drugs, which can directly kill bacteria, but with the widespread use of azole drugs, drug resistance is becoming more and more serious. ...

Claims

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Application Information

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IPC IPC(8): C07D209/88A61P31/10
CPCA61P31/10C07D209/88A61K31/40A61K31/495C07D209/82C07D295/02
Inventor 邓音乐黄珺珺黄小容叶秋棉贺飞赵朔黄钰童
Owner SOUTH CHINA AGRI UNIV
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