Beta-lactam compound as well as preparation method and application of beta-lactam compound

A technology for lactams and compounds, which is applied in the field of preparation of the above-mentioned β-lactam compounds, can solve the problems of antibacterial reduction and other problems, and achieve the effect of enhancing antibacterial activity and good antibacterial activity

Inactive Publication Date: 2014-08-06
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, with the continuous emergence of drug-resistant bacteria, the antibacterial activity of existing antibiotics against new bacteria is gradually reduced, so it is necessary to develop a new type of β-lactam compound with good antibacterial activity

Method used

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  • Beta-lactam compound as well as preparation method and application of beta-lactam compound
  • Beta-lactam compound as well as preparation method and application of beta-lactam compound
  • Beta-lactam compound as well as preparation method and application of beta-lactam compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] A kind of preparation method of 7-(4-parahydroxylaminobenzenesulfonyl)-3-desacetoxy cephalosporanic acid, adopts following steps to obtain:

[0022] Add 10ml of water, 10ml of acetone and 30ml of 0.76mol / L NaHCO to the four-necked flask in sequence 3 Solution, after being cooled to-5 ℃, add 2.14g7-ADCA (10mmol) again, carry out reaction; After reacting for half an hour until the solution is clear, keep the temperature constant, slowly drop 4.42g p-nitrobenzenesulfonyl chloride ( 0.02mol), reacted for 3h and filtered; at room temperature, distilled off the acetone in the filtrate, washed the solution with 30ml ethyl acetate for 3 times; then transferred the solution to a 200ml beaker, and added 50ml Ethyl acetate, and then drop an appropriate amount of saturated oxalic acid solution to adjust the pH value of the solution. When the pH of the solution is 2-3, separate the organic phase; wash the organic phase with 10ml saturated saline for 3 times, and then wash the organi...

Embodiment 2

[0026] A kind of preparation method of 6-(4-parahydroxylaminobenzenesulfonyl) penicillanic acid, adopts following steps to obtain:

[0027] Add 10ml of water, 10ml of acetone and 30ml of 0.76mol / L KHCO to the four-necked flask in sequence 3 Solution, after being cooled to-5 ℃, add 2.14g6-APA (10mmol) again, carry out reaction; After reacting half an hour to solution clarification, keep temperature constant, in solution, slowly drop into 4.42g p-nitrobenzenesulfonyl chloride ( 0.02mol), reacted for 3h and filtered; at room temperature, distilled off the acetone in the filtrate, washed the solution with 30ml ethyl acetate for 3 times; then transferred the solution to a 200ml beaker, and added 50ml Ethyl acetate, then add dropwise an appropriate amount of saturated oxalic acid solution to adjust the pH value of the solution, when the pH of the solution is 2-3, carry out liquid separation operation; the organic phase after liquid separation is washed 3 times with 10ml saturated sa...

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Abstract

The invention discloses a beta-lactam compound, and the chemical structural formula of the beta-lactam compound is shown in the specification. The invention also discloses a preparation method and an application of the beta-lactam compound. The beta-lactam compound disclosed by the invention, which has a feature pharmacophores (p-aminobenzenesulfonamide) of sulfonamides drugs and a feature pharmacophore (6-APA or 7-ADCA) of beta-lactams drugs, is obtained by synthesizing on the basis of combination principles. Since the pharmacophores of both drugs are compatible in a molecule, the compound disclosed by the invention has not only the drug properties of sulfonamides drugs and beta-lactams drugs, but also a synergistic effect between two pharmacophores, and thus the antibacterial activity of the compound disclosed by the invention is effectively enhanced and the toxic and side effect of drugs on the human body is reduced. The preliminary studies show that the compound disclosed by the invention exhibits good antibacterial activity against Pseudomonas aeruginosa and is comparable to carbenicillin.

Description

technical field [0001] The present invention relates to a β-lactam compound, and also relates to a preparation method and application of the β-lactam compound. Background technique [0002] Sulfa drugs were born in 1932 and are the earliest synthetic antibacterial drugs. Sulfonamides are stable in nature, easy to use, cheap, and easy to store for a long time. Sulfa drugs have definite curative effect and can inhibit most Gram-positive bacteria and some Gram-negative bacteria. They also have a good inhibitory effect on some fungi. The most sensitive ones are Streptococcus, Streptococcus pneumoniae and so on. In the history of human anti-infection, it has been widely used to treat diseases caused by the above-mentioned pathogenic microorganism infection, and occupies an important position in the development history of antibacterial drugs. [0003] β-lactam antibiotics refer to antibiotics containing β-lactam rings in their molecules. They are the largest class of antibiotic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/16C07D501/06C07D499/21C07D499/12A61K31/545A61K31/43A61P31/04
CPCC07D499/12C07D499/21C07D501/06C07D501/16
Inventor 蒋立建唐赛杰何慧顾美萍
Owner SOUTHEAST UNIV
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