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Application of small molecule compounds as adjuvant in preparation of antifungal drugs

A technology of small molecular compounds and antifungal drugs, applied in the field of medicine, can solve the problems of high difficulty, few types and great difficulty in research and development of antifungal drugs

Active Publication Date: 2016-10-12
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, there are few types of antifungal drugs, and there is little room for choice. Generally, they have strong toxic and side effects, and the systemic use is limited. Moreover, the resistance of fungi to antifungal drugs is becoming more and more common, and the development of new antifungal drugs is difficult. significantly higher than antibacterial drugs
These difficulties make clinical control of fungal infections more and more difficult

Method used

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  • Application of small molecule compounds as adjuvant in preparation of antifungal drugs
  • Application of small molecule compounds as adjuvant in preparation of antifungal drugs
  • Application of small molecule compounds as adjuvant in preparation of antifungal drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: Screening of Small Molecular Compounds

[0026] 1. Test material:

[0027] Amphotericin B

[0028] Alamarblue reagent

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Abstract

The invention discloses an application of a kind of small molecule compounds as an adjuvant in the preparation of antifungal drugs. After 51,520 small molecule compounds in a national compound sample bank are subjected to high-throughput screening, the result shows that when small molecule compounds as shown in a formula I to a formula X independently act on a candida albicans biological membrane, the inhibition ratio is almost zero, but when the small molecule compounds are used with conventional antifungal drugs such as amphotericin B, fluconazole or caspofungin, the remarkable synergism is achieved, the efficacy of the conventional antifungal drugs is improved by 30% or above, the use dosage of the conventional antifungal drugs is reduced, and the inhibiting effect of the antifungal drugs to drug resistance fungi is improved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of a class of small molecular compounds as adjuvants in the preparation of antifungal drugs. Background technique [0002] In recent years, the crisis of antibiotic resistance has received more and more global attention. Candida albicans (Saccharomyces albicans, formerly known as Candida albicans) is an important part of the normal microbiota of humans (mouth, gastrointestinal tract, vagina, and urinary tract), and it is also the most common opportunistic fungus in humans and the cause of nosocomial infections. One of the pathogenic bacteria that can cause infection of the body surface and deep tissues and organs (viscera or implanted devices) under certain conditions. Especially in human immunodeficiency patients, the mortality rate caused by systemic infection caused by Candida albicans is as high as 29%-76%. In nosocomial infection, the death rate caused by ...

Claims

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Application Information

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IPC IPC(8): A61K31/165A61K31/428A61K31/426A61K31/437A61P31/10A61K38/12A61K31/7048A61K31/4196A61K47/22A61K47/18
CPCA61K31/165A61K31/4196A61K31/426A61K31/428A61K31/437A61K31/7048A61K38/12A61K47/18A61K47/22A61K2300/00
Inventor 亓庆国郭静张晟
Owner SHANDONG UNIV
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