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Novel antibacterial application of NPS-2143

A technology of NPS-2143 and its application, which is applied in the direction of antibacterial drugs, nitrile/isonitrile active ingredients, etc.

Inactive Publication Date: 2018-08-21
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But so far, the compound has not been used in the report of antibacterial application

Method used

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  • Novel antibacterial application of NPS-2143

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Example 1. NPS-2143 can inhibit the growth of Staphylococcus aureus.

[0012] Pick a single colony of ATCC 33591 or ATCC 25923 or ATCC 6538 and inoculate it in 5 mL of MHB medium, and culture overnight at 37°C and 250 rpm. Transfer the overnight culture solution to 5 ml MHB medium at a ratio of 1:100, 37 °C, 250 rpm, 3-4 h (cultivate until OD 600 =0.5~0.6). Dilute the bacterial solution to 1×10 with MHB medium 5 CFU / mL.

[0013] Using the double dilution method for high-throughput screening, dilute the drug comparison into a series of concentrations (such as: 64, 32, 16, 8, 4, 2, 1, 0.5, 0.25, 0.125, 0.0625 μg / mL) and Mix it with the same amount of bacterial dilution and place it in a 96-well plate. Make 3-4 duplicate holes for each concentration of drug, and use linezolid as a positive control, and set a blank control without drug. Bacteria were cultured in the incubator for 24 hours, and the OD of each well was detected 600 value, calculate the inhibition rate, ...

Embodiment 2

[0017] Example 2. Time-killing curves of different concentrations of NPS-2143.

[0018] A single colony of ATCC 33591 or ATCC 25923 was picked and inoculated in 5 mL of MHB medium, and cultured overnight at 37 °C and 250 rpm. Transfer the overnight culture solution to 5 mL MHB medium at a ratio of 1:100, 37 °C, 250 rpm, 3-4 h (cultivate to OD 600 =0.5~0.6). Dilute the bacterial solution to 1×10 with MHB medium 5 CFU / mL, take 3 mL of the diluted bacterial solution and add it to the test tube. Add the optimal compound with the final concentration of 0 MIC, 1 / 4 MIC, 1 / 2 MIC, 1 MIC, 2 MIC, 4 MIC to each test tube respectively, and culture for 0 h, 2 h, 4 h, 6 h, 8 h , 12 h, 24 h, 36 h, 48 h, and 72 h were sampled and measured, and the bacterial solutions obtained at different time points were diluted by 10 -3 、10 -6 、10 -9 times, apply the bacterial solution on the MHA, place it in a 37°C incubator and incubate for 24 hours, and the final colony count is expressed in log10 / ...

Embodiment 3

[0020] Example 3, NPS-2143 can inhibit the growth of Staphylococcus aureus persistent bacteria.

[0021] Ciprofloxacin was used to control the time to construct the persistent bacteria model. The preserved ATCC 33591 was cultured overnight in 5 mL of MHB medium at 37 °C and 250 rpm. Transfer the overnight culture solution to 10 mL of MHB medium at a ratio of 1:1000, add 3 μg / mL ciprofloxacin control group and blank control group, 37 ℃, 250 rpm, at 0 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 24 h to measure OD 600 value, and the bacterial solution was diluted by 10 -3 、10 -6 、10 -9 times, the smeared bacteria solution was placed on the MHA, placed in a 37°C incubator for 24 hours and counted, with time as the abscissa and Log (CFU / mL) as the ordinate to draw a graph to confirm the time point for the establishment of the persistent bacteria model.

[0022] The preserved ATCC 33591 was cultured overnight in 5 mL of MHB medium at 37 °C and 250 rpm. The overnight culture solution wa...

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Abstract

The invention discloses novel antibacterial application of NPS-2143. The systematic name of NPS-2143 is 2-chloro-6-[(2R)-3-[[1,1-dimethyl-2-(2-naphthyl)ethyl]amino]-2-hydroxypropoxy]benzonitrile. Theinvention provides application of NPS-2143 in inhibition of Gram-positive bacteria and persistent bacteria thereof. According to the results of determination of inhibitory activity against the growthof a plurality of Gram-positive bacteria, NPS-2143 has good inhibitory activity against common Gram-positive bacteria such as MSSA strains (ATCC 25923), MSSA strains (ATCC 6538) and MRSA strains (ATCC33591). NPS-2143 has superiority in inhibition of sensitive Gram-positive bacteria and drug-resistant Gram-positive bacteria and in resistance of persistent bacteria compared with ciprofloxacin (CPFX), and shows good application prospects in the development of novel antibacterial drugs.

Description

technical field [0001] The invention relates to the new application of NPS-2143 compound as antibacterial, belonging to the field of biomedicine. Background technique [0002] Gram-positive bacteria are bacteria that can be stained dark blue or purple with a Gram stain, have thicker cell walls, and are rich in peptidoglycan. Gram-positive bacteria account for a high proportion of clinical infections. Staphylococcus aureus, Bacillus anthracis, and Diplococcus pneumoniae are representatives of Gram-positive pathogens, which can cause local suppurative infection, pneumonia, pericarditis, and other diseases . [0003] Staphylococcus aureus is an important human and animal pathogenic bacteria, which can cause various types of infectious diseases, and is mainly treated clinically by antibiotics. However, with the global spread of drug-resistant strains, especially methicillin-resistant Staphylococcus aureus (MRSA), MRSA has become one of the most difficult ESKAPE pathogens. Dru...

Claims

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Application Information

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IPC IPC(8): A61K31/277A61P31/04
CPCA61K31/277
Inventor 罗有福杨涛魏于全
Owner SICHUAN UNIV
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