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Polyphosphate kinase targeting inhibitor P8

A technology of polyphosphate and inhibitors, which is applied in the direction of anti-toxins, medical preparations containing active ingredients, anti-bacterial drugs, etc., and can solve serious problems such as drug resistance

Inactive Publication Date: 2019-09-24
PEKING UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Urinary tract infection caused by UPEC is mainly treated with antibiotics, but with the widespread use of antibiotics, the drug resistance of UPEC is becoming more and more serious

Method used

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  • Polyphosphate kinase targeting inhibitor P8
  • Polyphosphate kinase targeting inhibitor P8
  • Polyphosphate kinase targeting inhibitor P8

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0031] 1. Materials

[0032] Strains and cell lines

[0033] Uropathogenic Escherichia coli CFT073 and human bladder cancer epithelial cell line 5637 were kindly donated by Professor Huang Shenghe from Children's Hospital of USC Los Angeles, and the ppk1 knockout strain (Δpk1) of CFT073 was constructed and preserved in our laboratory.

[0034] 2. Reagents

[0035] LB medium was purchased from OXOID Company in the UK; PBS powder was purchased from Boster Biological Company; DMSO was purchased from Sigma Company; RPMI-1640 medium, fetal bovine serum (FBS) and trypsin were purchased from Gibco Company; 30% hydrogen peroxide The solution was purchased from Guangzhou Zhongnan Chemical Reagent Company; acridine orange (AO) was purchased from Solarbio Company; absolute ethanol, glacial acetic acid, and chloroform were purchased from Guangzhou Panyu Liqiang Chemical.

[0036] 3. Method

[0037] 3.1 Computer virtual screening

[0038] use Suite 2019 prepared the crystal structur...

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PUM

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Abstract

The invention relates to a polyphosphate kinase targeting inhibitor. The polyphosphate kinase targeting inhibitor is a compound P8, wherein the molecular formula is C13H8O2N3Cl, and the structural formula is shown in a formula (I). The polyphosphate kinase targeting inhibitor can inhibit the resistance of uropathogenic escherichia coli to oxidation stress, inhibit the formation of a uropathogenic escherichia coli biofilm, and inhibit the invasive function of the uropathogenic escherichia coli on urothelial cells. The polyphosphate kinase targeting inhibitor is expected to be prepared into a drug for treating urinary tract infections.

Description

technical field [0001] The invention belongs to the technical field of targeting compounds, and more specifically, the invention relates to a polyphosphate kinase targeting inhibitor. Background technique [0002] Urinary tract infection is one of the clinical frequently-occurring infectious diseases, and its pathogenic bacteria include Escherichia coli, Enterococcus, Proteus mirabilis, Klebsiella pneumoniae, Pseudomonas aeruginosa and fungi, among which Escherichia coli Escherichia is the most common. Escherichia coli that cause urinary tract infections are collectively referred to as uropathogenic Escherichia coli (UPEC). Clinically, antibiotics are the main treatment for urinary tract infection caused by UPEC, but with the widespread use of antibiotics, the drug resistance of UPEC is becoming more and more serious. UTIs caused by UPEC are also characterized by female susceptibility and repeated infections. If not effectively treated, it can further cause serious consequ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D235/18A61K31/4184A61P13/02A61P31/04A61P39/06
CPCC07D235/18A61P13/02A61P31/04A61P39/06Y02A50/30
Inventor 金宏威彭亮杨立鑫张亮仁刘振明
Owner PEKING UNIV
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