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Purpose of L-cysteine compound for restraining new delhi metallo (NDM)-1 activity

A technology of cysteine ​​and compounds, which is applied in the field of pharmacy, can solve the problems of undiscovered L-cysteine ​​compounds and achieve the effects of treating drug-resistant bacterial infections, eliminating hydrolysis, and good drug application prospects

Inactive Publication Date: 2013-06-05
TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The application of L-cysteine ​​compounds in inhibiting bacterial activity has not been found so far

Method used

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  • Purpose of L-cysteine compound for restraining new delhi metallo (NDM)-1 activity
  • Purpose of L-cysteine compound for restraining new delhi metallo (NDM)-1 activity
  • Purpose of L-cysteine compound for restraining new delhi metallo (NDM)-1 activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1 Determination of NDM-1 activity inhibited by N-benzyloxycarbonyl-L-cysteine

[0053]

[0054] The N-benzyloxycarbonyl-L-cysteine ​​used was purchased from Bailingwei with a purity of 98%.

[0055] Dissolve N-benzyloxycarbonyl-L-cysteine ​​(4 mg) in 95% DMSO double-distilled water (156.7 μL) to prepare a solution with a concentration of 100 mM, then place the solution in a 1.5 ml ep tube, and Store at 4°C.

[0056] Then according to the above activity test method step 5 (preliminary screening of compound) and step 6 (IC of compound) 50 Determination of value) to carry out the operation, then take the concentration logarithm of N-benzyloxycarbonyl-L-cysteine ​​as the abscissa, and the residual activity fraction of NDM-1 as the ordinate to draw a curve, see image 3 . Finally, according to the curve, using GraphPad Prism version 5.0 software to calculate, the obtained IC 50 The value was 62.26±7.8 μM.

Embodiment 2

[0057] Example 2 Determination of NDM-1 Activity Inhibited by N-acetyl-L-cysteine

[0058]

[0059] The N-acetyl-L-cysteine ​​used was purchased from Bailingwei with a purity of 99%.

[0060] N-acetyl-L-cysteine ​​(4 mg) was dissolved in 95% DMSO double distilled water (245.1 μL) to prepare a solution with a concentration of 100 mM, and then the solution was placed in a 1.5 ml ep tube, at 4 Store at ℃.

[0061] Then operate according to the content described in step 5 and step 6 of the above activity test method, and then take the logarithm of the concentration of N-acetyl-L-cysteine ​​as the abscissa, and the remaining activity fraction of NDM-1 as the ordinate To draw a curve, see Figure 4 . Finally, according to the curve, using GraphPad Prism version5.0 software to calculate, the obtained IC 50 The value was 195.1±35 μM.

Embodiment 3

[0062] Example 3 Determination of NDM-1 activity inhibited by N-tert-butoxycarbonyl-L-cysteine

[0063]

[0064] The N-tert-butoxycarbonyl-L-cysteine ​​used has a purity of 98%.

[0065] Dissolve N-tert-butoxycarbonyl-L-cysteine ​​(4mg) in 95% DMSO (180.8μL) to prepare a solution with a concentration of 100mM, then place the solution in a 1.5ml ep tube, and store at 4°C Save it.

[0066] Then operate according to the content described in the above activity test method step 5 and step 6, then take the logarithm of the concentration of N-tert-butoxycarbonyl-L-cysteine ​​as the abscissa, and the residual activity fraction of NDM-1 is To draw a curve on the ordinate, see Figure 5 . Finally, according to the curve, the GraphPadPrism version 5.0 software is used to calculate the obtained IC 50 The value was 404.3±49.7 μM.

[0067] According to the above examples, it can be known that the compounds involved in the present invention can inhibit the activity of NDM-1, and can ...

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Abstract

The invention provides purpose of L-cysteine compound with a following general formula for restraining new delhi metallo (NDM)-1 activity in medicine. R is C1-C4 carbalkoxy or aromatic oxygen carbonyl or C1-C4 alkyl acyl. The compound has the function on restraining NDM-1 activity.

Description

technical field [0001] The present invention relates to the field of pharmacy, in particular to the use of L-cysteine ​​compounds. Background technique [0002] In the 1950s and 1960s, known as the "golden age" of antibiotics, about 7 million people died of infectious diseases worldwide every year, and this number rose to 20 million by 1999. The main reason for the increase in the fatality rate is the difficulty in medication brought by drug-resistant bacteria. [0003] At present, the problem of bacterial resistance has become very serious. In developed countries, 5% to 10% of hospitalized patients have one or more infections. There are about 2 million patients with nosocomial infection in the United States every year, 90,000 people die, and the economic loss reaches 4.5 billion to 5.7 billion US dollars. In developing countries, the risk of nosocomial infection is 2 to 20 times higher than in developed countries. The incidence rate of nosocomial infection in our countr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/27A61K31/198A61P31/04
CPCY02A50/30
Inventor 饶子和陈悦杨诚娄智勇徐寅通白翠改李宁宁王静夏强
Owner TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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