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Application of substituted benzene guanidine derivative serving as polymyxins antibiotic potentiator

A polymyxin and derivative technology, applied in the field of biomedicine, can solve problems such as environmental pollution and the impact of the application of polymyxin antibiotics, and achieve a significant effect of drug resistance reversal

Active Publication Date: 2015-11-11
GUANGZHOU INSIGHER BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, due to the problem of bacterial resistance, the application of polymyxin antibiotics in actual production and life has been greatly affected
In production practice, a variety of drugs have been used in combination with polymyxin antibiotics in order to increase the efficacy of drugs. Experiments have proved that the therapeutic effects of these compatible drugs combined with polymyxin antibiotics are actually their inhibition of different infection strains. Combined results of effects without any synergistic effect on polymyxin antibiotics
In addition, these compatible drugs are either antibacterial agents or bactericides or chemical reagents with certain toxicity. Long-term combined use may cause new multidrug-resistant strains or cause serious pollution to the environment. Some compatible drugs have been approved by the European Union. Prohibit the use of rods as feed additives

Method used

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  • Application of substituted benzene guanidine derivative serving as polymyxins antibiotic potentiator
  • Application of substituted benzene guanidine derivative serving as polymyxins antibiotic potentiator
  • Application of substituted benzene guanidine derivative serving as polymyxins antibiotic potentiator

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1: Preparation of substituted benzoguanidine derivatives

[0041] Substituted benzoguanidine derivatives, its structural formula is as shown in formula (I):

[0042]

[0043] where: R 1 , R 2 , R 3 and R 4 H, CN, NO 2 , S(=O) 2 CH 3 , C(=O)OC 1 - 8 Straight chain or branched chain alkyl, halogen, C 1 - 8 Straight chain or branched chain alkyl, C 1 - 8 Straight chain or branched haloalkyl, O-C 1 - 14 Straight chain or branched chain alkyl, O-C 3 - 8 Cycloalkyl; O-CH 2 -Ph, O-Ph, S-C 1 - 14 Straight chain or branched chain alkyl, or, S-C 1 - 14 Straight chain or branched haloalkyl;

[0044] The halogen is F, Cl, Br or I;

[0045] The haloalkyl group refers to an alkyl group substituted by F, Cl, Br or I;

[0046] The O-CH 2 The phenyl in -Ph and O-Ph refers to the phenyl that is unsubstituted or substituted by 1, 2, 3, 4 substituents, and the substituents are selected from F, Cl, Br, I, C 3 - 8 Cycloalkyl, C 1 - 8 Straight chain o...

Embodiment 2

[0055] Example 2: Synergistic effect of substituted benzoguanidine derivatives on the inhibitory activity of colistin sulfate-sensitive Escherichia coli.

[0056] The substituted benzoguanidine derivative in this example is a substituted benzoguanidine derivative hydrochloride. That is, the test was carried out with substituted benzoguanidine derivative hydrochloride.

[0057]Test the minimum inhibitory concentration (MIC) in vitro of colistin sulfate and substituted benzoguanidine derivatives to Escherichia coli (sensitive to colistin sulfate, MIC value is less than 4.0ppm) by test tube double dilution method. When 20.0ppm substituted benzoguanidine derivatives, the minimum inhibitory concentration of colistin sulfate to corresponding bacterial strains in vitro (it was to use the combined use of substituted benzoguanidine derivatives and colistin sulfate as test drug, during the test, the concentration of substituted benzoguanidine derivatives Fixed at 20.0ppm, and colistin ...

Embodiment 3

[0063] Example 3 Synergistic effect of substituted benzoguanidine derivatives on the inhibitory activity of colistin sulfate-resistant Escherichia coli.

[0064] The substituted benzoguanidine derivative in this example is a substituted benzoguanidine derivative hydrochloride. That is, the test was carried out with substituted benzoguanidine derivative hydrochloride.

[0065] Test the in vitro minimum inhibitory concentration (MIC) of colistin sulfate and substituted benzoguanidine derivatives to colistin sulfate resistant Escherichia coli (to colistin sulfate drug resistance, MIC value greater than 4.0ppm) by test tube double dilution method, At the same time, the minimum inhibitory concentration of colistin sulfate to the corresponding strains was tested in vitro when 20.0 ppm substituted benzoguanidine derivatives were respectively contained in the culture. The results showed that all test strains were resistant to colistin sulfate and all tested substituted benzoguanidine...

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Abstract

The invention discloses application of a substituted benzene guanidine derivative serving as a polymyxins antibiotic potentiator. For the first time, the substituted benzene guanidine derivative is found to be capable of serving as the polymyxins antibiotic potentiator, especially serving as a synergist of a polymyxins antibiotic to inhibit sensitive strains and a drug resistance reversal agent of the polymyxins antibiotic. The invention further provides combined application of the substituted benzene guanidine derivative or a combination containing the same and the polymyxins antibiotic in preparation of compound drug preparations for people or animals to treat diseases caused by gram-negative bacterial infection. The invention further provides combined application of the substituted benzene guanidine derivative or a combination containing the same and the polymyxins antibiotic in preparation of forage-use growth-promoting feed additives for animal breeding in animal husbandry.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to the application of substituted benzoguanidine derivatives as polymyxin antibiotic synergists. Background technique [0002] The chemical synthesis and biological application research of diaminoguanidine, especially substituted benzoguanidine derivatives, started very early, and the main research results are as follows: US4310541A discloses substituted benzoguanidine derivatives for the treatment of trichomoniasis and anti-parasites in humans; US4575560A provides The substituted benzoguanidine derivatives are applied in the direction of agricultural production, and have antifeedant activity and control squamous insects to protect crops; the substituted benzoguanidine derivatives provided by US3992446 are used as anti-protozoal drugs, especially anticoccidial drugs; WO2014176636A1 provides a series of Substituted phenylguanidine derivatives are used in the treatment of bacter...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/155A61P31/04A23K1/16
CPCA61K31/155A61K38/12A23K20/195A23K50/10A23K50/20A23K50/30A23K50/40A23K50/50A23K50/75A61P31/04A61K2300/00A61K9/0056A23K20/111A23K50/60
Inventor 彭险峰覃宗华
Owner GUANGZHOU INSIGHER BIOTECHNOLOGY CO LTD
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