the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more
Image
Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
Smart Image
Examples
Experimental program
Comparison scheme
Effect test
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 inertsolvent, 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: petroleumether / 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-...
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More
PUM
Login to View More
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
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More
Application Information
Patent Timeline
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.
Login to View More 
Login to View More