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
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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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