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Compound and medicament for treating MRSA (Methicillin-resistant Staphylococcus Aureus) infection

A compound and combined technology, applied in the field of compounds and drugs for the treatment of MRSA infection, can solve the problem of low specificity and achieve the effect of high specificity and low side effects

Inactive Publication Date: 2013-10-23
上海交通大学医学院附属第三人民医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Aiming at the defect of low specificity in the treatment of MRSA infection by PACT, the present invention provides a compound, medicine, and preparation method thereof for treating MRSA infection

Method used

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  • Compound and medicament for treating MRSA (Methicillin-resistant Staphylococcus Aureus) infection
  • Compound and medicament for treating MRSA (Methicillin-resistant Staphylococcus Aureus) infection
  • Compound and medicament for treating MRSA (Methicillin-resistant Staphylococcus Aureus) infection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] In this example, the synthetic raw material is: 7-amino-3-chloromethyl-3-cefoxime-4-carboxylic acid p-methoxyphenyl methyl ester (7-amino-3-chloromethyl-3-cephen-4 -carboxylic acid p-methoxybenzyl ester, hereinafter referred to as ACLE), photosensitizer 5-(4′-carboxybutylamino)-9-diethylaminobenzothiaphenazine chloride (5-(4′-carboxybutylamino)-9-diethylaminobezo [a] phenothiazinium chloride, hereinafter referred to as EtNBS-COOH). The above-mentioned raw materials have been commercialized, such as Santa Cruz Company, Sigma Company, Merck Company, etc. can be purchased, or can also be prepared according to the existing technology.

[0065] refer to figure 1 , the steps of synthesizing the compound in this example are as follows:

[0066] step 1

[0067] Add 30 mg of ACLE chloride to the dichloromethane solvent, add 15 μl of tripropylamine, 12 μl of N-methylimidazole, and 15 mg of 4-aminothiophenol, and react in an ice bath to obtain the compound 1- 1.

[0068] step...

Embodiment 2

[0074] Under strict storage and use conditions, the introduced photosensitive group will not actively decompose, but in order to prevent the photosensitive group from decomposing without specific illumination, on the basis of Example 1, this example is in the target product A quencher is introduced to ensure product stability.

[0075] In this example, the synthetic raw material is: 7-amino-3-chloromethyl-3-cefoxime-4-carboxylic acid p-methoxyphenyl methyl ester (7-amino-3-chloromethyl-3-cephen-4 -carboxylic acid p-methoxybenzyl ester, hereinafter referred to as ACLE), photosensitizer 5-(4′-carboxybutylamino)-9-diethylaminobenzothiaphenazine chloride (5-(4′-carboxybutylamino)-9-diethylaminobezo [a] phenothiazinium chloride, hereinafter referred to as EtNBS-COOH), black hole quencher (Black Hole Quencher3, hereinafter referred to as BHQ3).

[0076] refer to figure 1 , the steps of synthesizing the compound in this example are as follows:

[0077] step 1

[0078] Add 30 mg o...

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PUM

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Abstract

The invention provides a compound and a preparation method thereof. The compound has a structure shown in a structural formula (I), wherein MRAS-expressed beta-lactamase can activate photosensitive groups in the compound provided by the invention, so as to generate active oxygen for exterminating MRAS without influencing a microbe and normal tissue which have unexpressed beta-lactamase, and therefore, the compound provided by the invention can achieve the beneficial effects of high efficiency, high specificity and less side effect, can be used as a photosensitizer for PACT treatment of MRSA infection and can provide a powerful tool for treating clinical patients with MRSA injection.

Description

technical field [0001] The invention relates to a medicine, in particular to a compound and medicine for treating MRSA infection. Background technique [0002] Staphylococcus aureus is a clinically common and highly toxic bacterium. Since the advent of penicillin, the infectious diseases caused by Staphylococcus aureus have been largely controlled, but with the widespread use of penicillin, some Staphylococcus aureus produce penicillin Enzyme, which can hydrolyze the β-lactam ring, shows resistance to penicillin. Scientists have developed a new semi-synthetic penicillin that is resistant to penicillinase, namely methicillin. In 1959, methicillin was used in clinical practice to effectively control the infection of Staphylococcus aureus enzyme-producing strains, but in 1961 Methicillin-resistant Staphylococcus aureus (MRSA) was first discovered in Jevons in the United Kingdom. Since its discovery, MRSA has infected almost all over the world and has become one of the importa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/14A61K41/00A61K31/5415A61P31/04
Inventor 姚敏傅秀军方勇俞为荣
Owner 上海交通大学医学院附属第三人民医院
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