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Thenylidene bishydroxycoumarin compound and application thereof

A technology of thiophene methylene dicoumarins and compounds, which is applied in the field of dicoumarins and their application in sterilization, and can solve toxic effects, no antibacterial activity, toxicity of coumarins, etc. problem, to achieve strong antibacterial effect and good antibacterial activity in vitro

Inactive Publication Date: 2015-04-22
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although there are a wide variety of artificially designed and synthesized coumarin compounds, the success rate of antibacterial effects in clinical practice is indeed very low.
On the one hand, the toxicity of coumarin compounds is the main reason why they cannot be applied to the whole body
The currently reported coumarin compounds have obvious toxic effects in rodents, and have species and site specificity, which are related to their metabolic pathways and polymorphisms of CYP2A6 enzymes
In addition, toxicity is also closely related to the dosage and route of administration, and oral administration and high-dose administration are more likely to produce toxic reactions
On the other hand, although the introduction of some nitrogen heterocycles such as pyrrole, thiazole, pyrazole, etc. into coumarin compounds has shown good antibacterial biological activity, so far no coumarin compounds with a dicoumarin structure have been reported. Antibacterial activity reported

Method used

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  • Thenylidene bishydroxycoumarin compound and application thereof
  • Thenylidene bishydroxycoumarin compound and application thereof
  • Thenylidene bishydroxycoumarin compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] The bacteriostasis test of compound in 9 that embodiment 1 synthesizes is as follows:

[0065] 1 material

[0066] 1.1 Experimental strains

[0067] as table 1 As shown, 2 strains of G + strains (S. aureus, S. epidermidis) and 3 strains of G - Bacterial strains (Pseudomonas aeruginosa, Salmonella typhimurium, Escherichia coli) were used in this part of the experiment, and the above-mentioned bacterial strains were all obtained from nation Provided by the Institute for the Control of Pharmaceutical and Biological Products of the Ministry of Health.

[0068] Table 1

[0069]

[0070]

[0071] 1.2 Main solution formula

[0072] 1.2.1 M-H broth medium

[0073] 2.5g M-H broth dry powder, add 125μl MgCl 2 solution (with Mg 2+ 10mg / ml) and 200μl CaCl 2 solution (with Ca 2+ 10mg / ml), then dilute to 100ml with deionized water, and autoclave.

[0074] 1.2.2 M-H agar medium

[0075] 3. 8g M-H agar medium dry powder, add 100ml distilled water, mix well, let i...

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Abstract

The invention relates to a thenylidene bishydroxycoumarin compound and its application. The structural formula of the compound is as shown in the formula I. The application is an application of the above compound used as an antibacterial agent of staphylococcus aureus and staphylococcus epidermidis.

Description

technical field [0001] The invention relates to coumarin compounds and applications thereof, in particular to dicoumarin compounds and their application in sterilization. Background technique [0002] Coumarin is an important class of aromatic oxygen heterocyclic compounds containing benzoα-pyrone structure, which has good thermodynamic and photochemical stability, is easy to carry out structural modification and can conveniently introduce various functional groups, intramolecular With a large conjugated system and strong intramolecular electron transfer capability, this special rigid fused ring structure makes it widely used in many fields such as food, fuel, spices, optoelectronic materials, medicine, pesticides, supramolecular recognition, etc. potential application. Especially in the field of medicine, they play an important role in anti-bacteria, anti-fungal, anti-cancer, anti-virus, anti-oxidation, anti-coagulation, anti-inflammation, etc. The related research is beco...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D409/14A61K31/381A61P31/04
CPCC07D409/14
Inventor 李侠李明凯罗晓星李靖李汾曲迪侯征周颖
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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