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Application of caffeic acid derivatives in the preparation of medicines for treating gonorrhea

A medicine and a technology for gonorrhea, applied in the application field of caffeic acid derivatives in the preparation of medicines for the treatment of gonorrhea, and can solve problems such as no reports of caffeic acid derivatives

Active Publication Date: 2022-05-03
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, there is no report in the prior art whether caffeic acid derivatives can be used for the treatment of gonorrhea

Method used

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  • Application of caffeic acid derivatives in the preparation of medicines for treating gonorrhea
  • Application of caffeic acid derivatives in the preparation of medicines for treating gonorrhea
  • Application of caffeic acid derivatives in the preparation of medicines for treating gonorrhea

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The in vitro activity of the compounds of the present invention can be evaluated according to the EU drug susceptibility test standard (EUCAST; www.eucast.org).

[0038] According to EU drug susceptibility test standards, the minimum inhibitory concentration (Minimal Inhibitory Concentration, MIC) of different pathogenic bacteria to the compounds of formula (2) to formula (7) of the present invention was detected by agar plate dilution method. Resuscitate bacteria from ultra-low temperature freezer, inoculate onto GC agar plate containing 1% Vitox, 37°C, 5% CO 2 , cultured upside down for 14-18 hours, and the bacteria were scraped to prepare the bacterial suspension (OD 600 = 0.01), draw 5 μ l of bacterial liquid with a micro-sampler and place samples on flat plates containing the compounds of the present invention at various concentrations, and air-dry naturally at 37 ° C, 5% CO 2 Cultivate under conditions for 24-48 hours, observe and record the MIC value. The MIC v...

Embodiment 2

[0042] Overnight cultured Neisseria gonorrhoeae (ATCC 49226) prepared as OD in GC broth 600 =1 bacterial suspension, get a certain amount of bacterial suspension and add in 12mL GC liquid culture medium containing 1% vitox (10 7 CFU / mL). After incubating it for 1 hour at 37° C. in a shaker at 200 rpm / min, the compound of formula (2) was added, and penicillin was used as a positive control.

[0043] At different time points, after sampling, dilute to an appropriate concentration, draw 100 μL of the diluted bacterial solution and spread it on a GC agarose plate, and place the plate at 37°C, 5% CO 2 Cultivate in an incubator for 24-48h, observe and record the number of clones (CFU).

[0044] The result is as figure 1As shown, the results are expressed as the mean ± SD of three biological replicates, and the dotted line indicates the lower limit of detection. Compared with penicillin, at 4*MIC (4*32μM) and 2*MIC (2*32μM) concentrations, the compound of formula (2) can effectiv...

Embodiment 3

[0046] The in vitro activity of the compounds of the present invention can be evaluated according to the EU drug susceptibility test standard (EUCAST; www.eucast.org).

[0047] According to EU drug susceptibility test standard, detect the minimum inhibitory concentration (Minimal Inhibitory Concentration, MIC) of the compound of formula (2) of the present invention with the agar plate dilution method of clinical isolates of gonorrhoeae (n=100), the 100 strains of gonorrhea clinical Isolates contained gonorrhoeae resistant to ceftriaxone, cefixime, azithromycin, penicillin, ciprofloxacin, and tetracycline. Resuscitate bacteria from ultra-low temperature freezer, inoculate onto GC agar plate containing 1% Vitox, 37°C, 5% CO 2 , cultured upside down for 14-18 hours, and the bacteria were scraped to prepare the bacterial suspension (OD 600 = 0.01), draw 5 μ l of bacterial liquid with a micro-sampler and place samples on flat plates containing the compounds of the present inventio...

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PUM

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Abstract

The invention discloses the application of caffeic acid derivatives in the preparation of medicines for treating gonorrhea. The caffeic acid derivatives are shown in formula (I). The compound of formula (2) in the caffeic acid derivatives of the present invention has extremely strong bactericidal activity against gonorrhoeae in vitro, indicating that it has broad application prospects in the preparation of drugs for treating infectious diseases caused by gonorrhea.

Description

technical field [0001] The invention relates to the field of antibacterial drugs, in particular to the application of caffeic acid derivatives in the preparation of drugs for treating gonorrhea. Background technique [0002] Humans are the only host of Neisseria gonorrhoeae, and infection with Neisseria gonorrhoeae usually causes sexually transmitted diseases. At present, Neisseria gonorrhoeae is resistant to most of the antibiotics that have been used as empirical drugs, such as penicillin, tetracycline, sulfonamides, trimethoprim, (fluoro) Both quinolones and macrolides have evolved drug resistance. [0003] Ceftriaxone is an internationally recognized first-line empirical drug. The ceftriaxone resistance rate was 0.1% in the United States in 2013-2014, 0.25% in Europe in 2014, and 0.6% in Australia in 2014. However, The hyposensitivity rate of ceftriaxone in my country from 2013 to 2015 has reached as high as 10.8%. As a result, the status of ceftriaxone as a first-line d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/216A61P31/04
CPCA61K31/216A61P31/04
Inventor 斯戴·樊德冯西蒙·杜特怀勒张江临杨帆严景孙雨吉
Owner ZHEJIANG UNIV