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New antifungal compound, preparation method and application

A compound and composition technology, applied in antifungal agents, organic chemistry, fermentation, etc., can solve problems such as narrow antibacterial spectrum, low safety, and increased drug resistance

Inactive Publication Date: 2009-12-09
NORTH CHINA PHARMA GROUP CORP +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, because of side effects such as nephrotoxicity, it is pointed out that there are safety problems (Gallis et al., Rev. Infect. Dis. Vol 12, p309-329, 1990), and flucytosine drugs also have low safety and drug-resistant bacteria etc.
[0005] On the other hand, azole drugs are considered to have a wide range of safety and low side effects, but they have a problem of narrow antibacterial spectrum, so their effectiveness against serious conditions is low, and drug resistance is considered to be increasing

Method used

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  • New antifungal compound, preparation method and application
  • New antifungal compound, preparation method and application
  • New antifungal compound, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] The preparation of embodiment 1 compound NCC00646

[0062] (1) Cultivation of strain NCC00646

[0063] Single spores of Penicillium implicatum were cultured on fresh malt extract agar (MEA) slant at 24°C for 5 days. The cultured slant was made into 10 ml of spore suspension containing 0.01% Tween 80. Spread 0.5 ml of spore suspension evenly on a plate containing malt extract agar (MEA). After culturing for 5 days, scrape the spores on the plate with a sterile loop, suspend them in sterile distilled water, and inoculate them into organisms containing 15 kg of wheat bran. 7 days in the reactor. Culture container (made of stainless steel) 200×80×17cm

[0064] (2) Extraction and purification of compound NCC00646

[0065] A part (2 kg) of the above culture was first extracted with 2L of 67% acetone aqueous solution to obtain a crude extract. Filter and distill off acetone, then extract with 1.5L ethyl acetate. Evaporation of the ethyl acetate extract gave 6.8 g of crud...

Embodiment 2

[0067] Example 2: Antifungal Activity Determination of Compound NCC00646

[0068] For the antifungal activity of the compound (1) obtained in Example 2, the minimum inhibitory concentration to fungal strains was determined by the liquid concentration dilution method. The fungus was cultured in YNBP medium (buffered yeast nitrogen base, containing 0.5% glucose, produced by DIFCO method) at 28°C for 48 hours. The results are shown in Table 1.

[0069] Table 1. Antifungal activity of compound (1)

[0070] test strain

[0071] Table 1 shows that the compound (1) of the present invention has good antifungal activity.

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Abstract

This invention describes the compound NCC00646 having the molecular formula (1) and its medicinal salt, which has good antifungal activity. This invention also describes a process for preparing the compound NCC00646, and the application of the drugs containing the compound (1) in the preparation of the drugs that can treat and / or prevent mycotic infection.

Description

technical field [0001] The present invention relates to a new compound with antifungal activity, its preparation method and use. More specifically, the present invention discloses a compound of molecular formula (1), a pharmaceutical composition containing it, a method for preparing the compound by fermentation of microorganisms, a new microorganism used, and the preparation of the compound and its pharmaceutical composition Use in therapeutic and / or prophylactic antifungal agents. [0002] Background technique [0003] After 1950, research related to antibiotics developed rapidly and became widely popularized, and many therapeutic drugs for various infectious diseases were developed. On the other hand, in recent years, there has been an increase and aggravation of deep fungus caused by Candida, Aspergillus, Cryptococcus and other fungi. These phenomena are related to leukemia, malignant lymphoma, immunosuppression caused by HIV infection, and anticancer drugs. It is cl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/14C12P17/10A61K31/407A61P31/10C07D209/00C07D259/00
Inventor 张华董悦生谷匡人饭田真依子
Owner NORTH CHINA PHARMA GROUP CORP
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