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Compound with antibacterial synergism as well as preparation method and application thereof

A compound and chemical formula technology, applied in the field of compounds with antibacterial synergistic effect and their preparation, can solve problems such as inability to cure, can not catch up with the speed of generation of drug-resistant bacteria, etc., to achieve the effect of improving antibacterial effect

Inactive Publication Date: 2014-01-01
SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, it is precisely because of this wide application that it leads to the rapid emergence of drug-resistant bacteria, and even the generation of super-resistant bacteria that cannot be cured by drugs.
Now people mainly solve this problem by developing new and more powerful antibiotics. However, the birth of a new antibiotic takes time. Obviously, the speed of the birth of this new drug cannot catch up with the speed of the emergence of drug-resistant bacteria.

Method used

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  • Compound with antibacterial synergism as well as preparation method and application thereof
  • Compound with antibacterial synergism as well as preparation method and application thereof
  • Compound with antibacterial synergism as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0114] Embodiment 1: the synthesis of p-dimethylaminobenzaldehyde

[0115] In a 100ml three-necked flask, add 4.9g (0.032mol) of phosphorus oxychloride, and slowly add 2.5g (0.031mol) of DMF dropwise under ice bath. 3.66g (0.03mol) N,N-dimethylaniline (10min), after dropping, move the reaction solution to a boiling water bath for 2 hours, after the reaction, pour the reaction solution into 20ml of ice water, and oxidize it with 30% hydrogen The sodium solution was adjusted to PH=4, left to stand for crystallization, and suction filtered the next day to obtain a light yellow or nearly colorless solid, which was recrystallized with 30ml of ethanol-water (1:2.5V / V) to obtain the product p-dimethylaminobenzaldehyde .

Embodiment 2

[0116] Embodiment 2: the synthesis of 2,4-dihydroxyacetophenone

[0117] Add 11.00g (0.1mol) of resorcinol and 30ml of glacial acetic acid in sequence to a 100ml three-necked flask equipped with a condenser, agitator, and a thermometer, raise the temperature to 145°C, and react at a constant temperature for 5 hours. After the reaction is complete, pour the reaction solution into 50ml of dilute hydrochloric acid (1:9), static crystallization, suction filtration, and recrystallization with ethanol-water (1:9V / V). In 2,4-dihydroxyacetophenone.

Embodiment 3

[0118] Example 3: Synthesis of 4-dimethylamino-2, 4-dihydroxychalcone

[0119] in N 2 Under protection, add 1.52g (0.010mol) 2,4-dihydroxyacetophenone, 1.94g (0.013mol) p-dimethylaminobenzaldehyde, DMSO 3ml, piperidine 1ml, Heat the oil bath to 150°C and react for 10 minutes. After the reaction is complete, pour the reaction solution into 50ml of 10% sodium hydroxide solution, filter with suction, acidify the filtrate with concentrated hydrochloric acid to PH=1-2, stand for crystallization, and filter with suction. The obtained solid was recrystallized from 15 ml of ethanol to obtain 1.60 g of 4-dimethylamino-2□,4□-dihydroxychalcone as a yellow solid, with a yield of 56.5%. 1 HNMR (400MHz, Acetone-d 6):δ3.13(s,6H,4-CH 3 );6.42(d,1H,3′-H);6.52(dd,J=8.9Hz,1H,5′-H);6.85(d,J=8.9Hz,2H,3-H,5-H) ,7.73(d,J=15.2Hz,1H,a-H);7.77(d,J=8.9Hz,2H,2-H,6-H);7.91(d,J=15.2Hz,1H,b-H);8.21 (d,J=8.9Hz,1H,6′-H);9.45(s,1H,4′-OH);13.92(s,1H,2′-OH)

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Abstract

The invention provides a compound with antibacterial synergism as well as a preparation method and application thereof. The compound has stronger antibacterial synergism, can remarkably improve antibacterial effect, especially for drug-resistant strains while being combined with antibacterial drugs for use. Especially in case of being combined with macrolide antibiotics and the like for use, the compound achieves antibacterial synergism, can assist antibiotics to restrain or kill sensitive bacteria and drug-resistant bacteria, for example staphylococcus aureus which is sensitive and drug-resistant to erythromycin. By adopting the compound and a pharmaceutically acceptable carrier, a pharmaceutical composition and a medicinal preparation can be prepared and antibacterial drug synergist can also be prepared.

Description

technical field [0001] The invention belongs to the fields of chemistry and medicine, and relates to a compound with antibacterial and synergistic effects and a preparation method thereof. Background technique [0002] The development of antibiotics and antibacterial drugs is the greatest contribution in the history of human drug development in the last century. Antibiotics are not only used in the clinical treatment of diseases caused by human bacterial infections, but also in many fields such as animal husbandry and aquaculture. However, it is precisely because of this wide application that the rapid emergence of drug-resistant bacteria, and even the generation of super-resistant bacteria that cannot be cured by drugs. Now people mainly solve this problem by developing new and more powerful antibiotics. However, the birth of a new antibiotic takes time. Obviously, the speed of the birth of this new drug cannot catch up with the speed of the emergence of drug-resistant bac...

Claims

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Application Information

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IPC IPC(8): C07C225/22C07C221/00C07C69/24C07C67/08A61K31/222A61P31/04
Inventor 戴康袁琳温超
Owner SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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