Uses of thiazole-based compound as antibacterial synergist

A technology of compounds and uses, applied in the field of medicine, can solve problems such as macro-nephrotoxicity and neurotoxicity

Active Publication Date: 2018-01-26
SHANGHAI INST OF PHARMA IND +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, on the one hand, due to its greater nephrotoxicity and neurotoxicity, on the other hand, due to the advent of carbapenem antibiotics

Method used

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  • Uses of thiazole-based compound as antibacterial synergist
  • Uses of thiazole-based compound as antibacterial synergist
  • Uses of thiazole-based compound as antibacterial synergist

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0139] Preparation method of the compound of the present invention

[0140] The compound represented by the general formula (I) of the present invention can be prepared by the following method, but the conditions of the method, such as reactant, solvent, base, amount of compound used, reaction temperature, reaction time required, etc. are not limited to the following Explanation. The compounds of the present invention can also be conveniently prepared by combining various synthetic methods described in this specification or known in the art, and such combinations can be easily performed by those skilled in the art to which the present invention belongs.

[0141] The compound represented by the general formula (I) of the present invention can be synthesized by the following method:

[0142] (1) In an inert solvent, a compound of formula A and a compound of formula B are reacted at a certain temperature (such as reflux) to obtain a compound of formula C. The compound of formula C rea...

Embodiment 1-30

[0165] Example 1-30: Preparation of Compound

Embodiment 1

[0166] Example 1 2-(4-Trifluoromethylbenzimidyl)-4-(4-methylphenyl)thiazole

[0167] 1.1 Preparation of N-(4-trifluoromethylphenyl)thiourea

[0168]

[0169] In a 100mL round-bottom flask, 12mmol of benzoyl chloride and 20mL of acetone were added, and then 12mmol of potassium thiocyanate was added. A large amount of white solid was formed in the reaction. After 15 minutes, when the reaction is over, the solid is filtered, and the filtrate is spin-dried to obtain a pale yellow liquid, which is directly put into the next reaction. A 100mL round bottom flask was charged with 10mmol of 4-trifluoromethylaniline, 30mL of ethyl acetate was dissolved, and the product prepared in the previous step was added to this solution, and heated to reflux for reaction. After the reaction was followed by TLC, the reaction solution was cooled to room temperature, the solvent was evaporated under reduced pressure, 10 mL ethanol and 10 mL 2N sodium hydroxide solution were directly added, and the reactio...

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PUM

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Abstract

The present invention relates to a compound with antibacterial synergy activity, a preparation and uses thereof, and particularly discloses a class of compounds represented by a formula (I), or optical isomers, cis-trans isomers or pharmaceutically acceptable salts thereof, wherein the compounds or the optical isomers, the cis-trans isomers or the pharmaceutically acceptable salts thereof can effectively enhance the antibacterial activity of antibiotics, and can be used for treating antibiotic-resistant bacteria. The formula (I) is defined in the specification.

Description

Technical field [0001] The present invention relates to the field of medicine, in particular to a class of compounds capable of enhancing the antibacterial activity of antibiotics, preparation methods and uses thereof. Background technique [0002] As the abuse of antibiotics in clinical and non-clinical applications has led to the proliferation and spread of bacterial resistance, the resulting "super bacteria" have become one of the main threats to global public health. At present, the "super bacteria" that are widely spread and spread worldwide are mainly ESKAPE, namely Enterococcus faecium (vancomycin-resistant Enterococcus faecium), Staphylococcusaureus (methicillin-resistant Staphylococcus aureus), Klebsiella pneumoniae (carbon blue) Mycene-resistant Klebsiella pneumoniae), Acinetobacter baumanii (pan-resistant Acinetobacter baumanii), Pseudomonas aeruginosa (multi-drug resistant Pseudomonas aeruginosa), and Enterobacter species (multi-drug resistant Enterobacter), A seriou...

Claims

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Application Information

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IPC IPC(8): A61K31/426A61K31/427A61K31/454A61K31/496A61K31/4439A61K38/12A61P31/04
Inventor 陈代杰徐晓勇邵雷李忠董晓景侯爽张骏梁王蓉
Owner SHANGHAI INST OF PHARMA IND
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