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A kind of broad-spectrum β-lactamase fluorescent substrate and its preparation method and application

A lactamase, fluorescent substrate technology, applied in biochemical equipment and methods, microbial determination/inspection, triarylmethane dyes, etc., can solve the problem of inability to specifically detect broad-spectrum beta-lactamase, etc. Achieving the effect of wide application space and practical value, few steps, and saving the patient's life

Active Publication Date: 2016-06-08
SHANGHAI BAIKE BIO TECH CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

GeneBLAze reagent is also based on fluorescence detection, however, this reagent can only be used to detect the presence of all β-lactamases indiscriminately, but cannot specifically detect the broad-spectrum β-lactamases that can degrade the third and fourth generations of cephalosporins

Method used

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  • A kind of broad-spectrum β-lactamase fluorescent substrate and its preparation method and application
  • A kind of broad-spectrum β-lactamase fluorescent substrate and its preparation method and application
  • A kind of broad-spectrum β-lactamase fluorescent substrate and its preparation method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] synthetic route

[0055]

[0056] Step A:

[0057] Cefotaxime (cefotaxime, 455.5 mg, 1.00 mmol) and toluenesulfonic acid (172.2 mg, 1.00 mmol) were dissolved in 5 mL of acetonitrile and 8 mL of aqueous solution; Diphenyldiazomethane (199.2 mg, 1.00 mmol , 1 equivalent); mixed and stirred at -20°C for 4 to 5 minutes until the characteristic purple color disappeared; after adding sodium hydroxide solution to the mixture to adjust the pH value to 9, it was extracted with ethyl acetate (50 ml); organic The layers were washed twice with water (15 mL), then dried over anhydrous calcium chloride; the solvent was removed using a rotary evaporator. The enrichment was separated and purified on a 50 g silica gel column with 30% n-hexane-ethyl acetate; the collected fractions were removed by rotary evaporation to obtain 500 mg of compound 1 as a white solid (yield 80%).

[0058] Proton NMR spectrum (deuterated chloroform, 600MHz) δ7.81(s,1H),7.50-7.29(m,10H),6.99(s,1H),6.83(s,...

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Abstract

The present invention provides a broad-spectrum β-lactamase fluorescent substrate used in a fluorescent detection method for detecting bacterial drug resistance in individuals, and its structure is as follows: Experimental results show that the fluorescent substrate C-2 provided by the present invention can accurately and qualitatively detect cephalosporin-resistant bacteria in different samples, and can be used in clinical or other detection fields to prepare corresponding diagnostic reagents or diagnostic kits. application space and practical value.

Description

technical field [0001] The invention relates to the field of drug synthesis, in particular to a fluorescent substrate that can be used to detect drug resistance of bacteria treated with broad-spectrum β-lactam antibiotics, and a preparation method and application thereof. Background technique [0002] Since humans first discovered β-lactam antibiotics represented by penicillin in the 1920s, they have become the first-line drugs for the treatment of bacterial infections and saved countless lives. Compared with other classes of antibiotics, β-lactam antibiotics have the characteristics of high curative effect and low toxicity. However, bacteria are also constantly evolving various resistance mechanisms. Currently, drug-resistant bacterial infections have become a global problem. Especially in China, India, and some other countries, due to the phenomenon of overuse of antibiotics, the emergence of super-resistant bacteria, resulting in the possibility of no cure cannot be ign...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K5/062C12Q1/34C12Q1/04
CPCC09B11/24C07K5/06026C12Q1/18C12Q1/34
Inventor 王郁生
Owner SHANGHAI BAIKE BIO TECH CO LTD
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