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Antibacterial synergist, preparation method and uses thereof

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

Pending 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 and its curative effect on Gram-negative bacterial infections, this drug was introduced in the late 1970s and early 1980s. terminate use

Method used

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  • Antibacterial synergist, preparation method and uses thereof
  • Antibacterial synergist, preparation method and uses thereof
  • Antibacterial synergist, preparation method and uses thereof

Examples

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preparation example Construction

[0176] The preparation method of the compound of the present invention

[0177] 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 the amount of reactant, solvent, base, compound used, reaction temperature, reaction time required, etc. are not limited to the following Explanation. The compounds of the present invention can also optionally be conveniently prepared by combining various synthetic methods described in this specification or known in the art, such combinations can be easily performed by those skilled in the art to which the present invention pertains.

[0178] Compound shown in general formula (I) of the present invention can be synthesized by following method:

[0179] (1) In an inert solvent, the compound of formula A is reacted with NBS at a certain temperature (such as 40-80°C). After the reaction is completed, the compound of formula B is obtained by ...

Embodiment 1-57

[0204] Example 1-57: Preparation of Compounds

Embodiment 1

[0205] Example 1 2-(4-trifluoromethylphenylimino)-4-(4-methylphenyl)thiazole

[0206] 1.1 Preparation of α-bromo-4-methylacetophenone

[0207]

[0208] Add 10mmol 4-methylacetophenone and 11mmol N-bromosuccinimide (NBS) to a 100mL round bottom flask, dissolve in 35mL ethyl acetate, then add 1g Amberlyst 15 ion exchange resin as a catalyst, and heat up the reaction solution Reaction at 40°C. After the reaction was followed by TLC, the reaction solution was filtered to remove Amberlyst 15 ion exchange resin, the filtrate was spin-dried, and separated by column chromatography (eluent: petroleum ether / ethyl acetate) to obtain pale yellow crystals with a yield of 53%. 1 H NMR (400MHz, CDCl 3 )δ7.88(d, J=8.2Hz, 2H), 7.28(d, J=8.1Hz, 2H), 4.43(s, 2H), 2.42(s, 3H).

[0209] 1.2 Preparation of 2-(4-trifluoromethylphenylimino)-4-(4-methylphenyl)thiazole

[0210]

[0211] Add 1mmol N-(4-trifluoromethylphenyl)thiourea and 1.05mmol α-bromo-4-methylacetophenone to a 25mL eggplant-...

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PUM

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Abstract

The present invention relates to an antibacterial synergist, a preparation method and uses thereof, and specifically discloses a compound represented by a formula (I) and having antibacterial synergyactivity, or an optical isomer, a cis-trans isomer or a pharmaceutically acceptable salt thereof, and a preparation method thereof. The present invention further discloses a medical composition containing the compound, and uses thereof. According to the present invention, the compound can effectively enhance the antibacterial activity of polymyxin B against Acinetobacter baumannii and Klebsiella pneumoniae, and can be used for the antibacterial treatment of pathogenic bacteria insensitive to polymyxin or having low bacterial inhibition activity. The formula (I) is defined in the specification.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular the invention relates to an antibacterial synergist and its preparation method and application. Background technique [0002] As the clinical and non-clinical abuse of antibiotics leads to the proliferation and spread of bacterial resistance, the resulting "super bacteria" has become one of the major threats to global public health. At present, the "super bacteria" that are widely spread and spread in the world are mainly: ESKAPE, namely Enterococcus faecium (vancomycin-resistant Enterococcus faecalis), Staphylococcusaureus (methicillin-resistant Staphylococcus aureus), Klebsiella pneumoniae (carbon blue Mycocene-resistant Klebsiella pneumoniae), Acinetobacter baumanii (pan-drug-resistant Acinetobacter baumannii), Pseudomonas aeruginosa (multidrug-resistant Pseudomonas aeruginosa), and Enterobacter species (multidrug-resistant Enterobacteriaceae), Seriously threaten human life and health...

Claims

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Application Information

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IPC IPC(8): C07D277/42C07D277/50C07D277/38C07D417/12C07D263/48C07D233/88A61K31/426A61K31/5377A61K31/506A61K31/421A61K31/4168A61K45/06A61P31/04
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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