Application of pyrroledione compound in preparation of antifungal drugs

A compound, antifungal technology, applied in the field of medicine, can solve problems such as high fatality rate and systemic infection

Active Publication Date: 2021-09-03
INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have found that Candida albicans usually does not cause disease on the mucous membrane surface of healthy human body, such as oral cavity, intestinal tract, etc., but in patients with compromised or suppressed immune system, such as chemotherapy patients, organ transplant patients or AIDS patients, Candida albicans will Causes severe systemic infection with a fatality rate of up to 40%

Method used

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  • Application of pyrroledione compound in preparation of antifungal drugs
  • Application of pyrroledione compound in preparation of antifungal drugs
  • Application of pyrroledione compound in preparation of antifungal drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1, the activity of formula I compound against Candida albicans

[0039] RPMI Media 1640: American Gibco company. Fluconazole, itraconazole and amphotericin B: Sigma-Aldrich, USA.

[0040] 1) Prepare bacterial liquid

[0041] Counted by hemocytometer, using RPMI Media 1640 medium to isolate Candida albicans sensitive person (Candida albicans SC5314), Candida albicans resistant strain (C.albicans 17#, C.albicans g5) (GongJiao, Wu Ju, Ikeh Melanie, Tao Li, Zhang Yulong, Bing Jian, Nobile Clarissa J., Huang Guanghua.Antifungal 1Activity of Mammalian Serum amyloid A1 against Candida albicans.Antimicrobial Agents and Chemotherapy.64(1):e01975-19), prepared as (2-5 )×10 5 cells / mL of bacterial fluid.

[0042] 2) preparation of test compound formula I solution

[0043] Compound formula I was prepared as a 4 mg / mL stock solution using sterile DMSO as a solvent, and then diluted in sequence with sterile DMSO to obtain concentrations of 2 mg / mL, 1 mg / mL, 500 μg / mL,...

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Abstract

The invention discloses a novel application of a compound as shown in a formula I. The new application is application of the compound shown in the formula I or pharmaceutically acceptable salt thereof in preparation of products for resisting fungi, especially candida albicans infection. According to the present invention, the anti-Candida albicans activity of the compound represented by the formula I is determined by using the microporous plate double dilution method, and the result shows that the compound represented by the formula I has good antibacterial activity on Candida albicans, such that the new drug for treating Candida albicans infection is expected to be explored.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of diketopyrrole compounds in the preparation of antifungal drugs. Background technique [0002] With the spread of chronic diseases such as hypertension, hyperlipidemia, and diabetes, the increase in the number of patients with cancer radiotherapy, chemotherapy, and organ transplantation, the widespread use of immunosuppressants, and the global epidemic of AIDS have led to the decline of human immunity and the onset of fungal infections. rate increased significantly. The antifungal drugs currently used clinically are mainly polyenes, allylamines, and flucytosine. However, the drug resistance of pathogenic fungi is becoming more and more serious, and the required dosage has to be gradually increased. Therefore, the research and development of new drugs for the treatment of fungal infection diseases is imperative. [0003] Candida is the most common opportunis...

Claims

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Application Information

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IPC IPC(8): A61K31/4015A61P31/10
CPCA61K31/4015A61P31/10
Inventor宋福行徐秀丽杨娜王龙
OwnerINST OF MICROBIOLOGY - CHINESE ACAD OF SCI