Application of a nitrogen-containing compound in the preparation of antifungal drugs

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

CN113318107BActive Publication Date: 2022-07-12INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Publication Date
2022-07-12

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Abstract

The present invention discloses new uses of nitrogen-containing compounds represented by formula I. The new application is the application of the compound represented by formula I or a pharmaceutically acceptable salt thereof in the preparation of a product for antifungal, especially anti-Candida albicans infection. The present invention adopts the microplate double dilution method to measure the anti-Candida albicans activity of the compound shown in formula I, and the results show that the compound shown in formula I has good bacteriostatic activity against Candida albicans, and is expected to explore new treatments Medications for Candida albicans infection.
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Description

technical field

[0001] The invention belongs to the field of medicine, in particular to the application of a nitrogen-containing compound in the preparation of antifungal medicines. 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, the human body's immune capacity has declined, and fungal infections have occurred. rate increased significantly. At present, the antifungal drugs in clinical use mainly include polyenes, allylamines, and flucytosines. Therefore, it is imperative to develop new drugs for the treatment of fungal infections.

[0003] Candida is the most common opportunistic pathogen among fungi, also known as Candida. It often parasitizes the human skin, oral cavity, vagina and intestinal mucosa, etc. When the immune fun...

Examples

Embodiment 1

[0037] Example 1. Activity of compound of formula I against Candida albicans

[0038] RPMI Media 1640: Gibco, USA. Fluconazole, itraconazole and amphotericin B: Sigma-Aldrich, USA.

[0039] 1) Prepare bacterial liquid

[0040] Counted by hemocytometer, the sensitive strain of Candida albicans (Candida albicans SC5314) and the resistant strain of Candida albicans (C.albicans 17#, C.albicans g5) (GongJiao, Wu Ju, Ikeh) were separately counted in RPMI Media 1640 medium. Melanie, Tao Li, Zhang Yulong, Bing Jian, Nobile Clarissa J., Huang Guanghua. Antifungal 1 Activity 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.

[0041] 2) Prepare a solution of compound formula I to be tested

[0042] With sterile DMSO as solvent, compound formula I is prepared as the mother liquor of 4mg / mL, and then sequentially diluted with sterile DMSO to obtain concentrations of 2mg / ...