Application of 3-mercaptopropionamide compounds

A technology for mercaptopropionamide and compound, which is applied in the field of 3-mercaptopropionamide compounds, can solve problems such as high in vitro sensitivity, and achieve the effects of improving curative effect, eliminating hydrolysis, and having good drug application prospects.

Inactive Publication Date: 2016-09-14
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 existence of NDM-1 is the molecular basis that causes NDM-1 super bacteria to be resistant to almost all β-lactam antibacterial drugs. At the same time, because bacteria have other drug resistance mechanisms, they are also resistant to aminoglycosides and quinolones. High in vitro sensitivity only to colistin and tigecycline

Method used

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  • Application of 3-mercaptopropionamide compounds
  • Application of 3-mercaptopropionamide compounds
  • Application of 3-mercaptopropionamide compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Determination of 3-mercapto-2-methyl-1-morpholine propionamide inhibiting NDM-1 activity

[0041]

[0042] Dissolve the above-mentioned 3-mercapto-2-methyl-1-morpholine propionamide (4 mg) in 95% DMSO (211.3 μL) to prepare a solution with a concentration of 100 mM, and then place the solution in a 1.5 ml ep tube , stored at 4°C.

[0043] Then according to the above activity test method step 5 (preliminary screening of compound) and step 6 (IC of compound) 50 Determination of the value) described in the operation. When the final concentration was 1.3mM, the inhibition rate of NDM-1 reached 51.44%

Embodiment 2

[0044] Example 2 Determination of 3-mercapto-2-methyl-N-phenylpropanamide inhibiting NDM-1 activity

[0045]

[0046] Dissolve the above-mentioned 3-mercapto-2-methyl-N-phenylpropanamide (4 mg) in 95% DMSO (204.8 μL) to prepare a solution with a concentration of 100 mM, and then place the solution in a 1.5 ml ep tube , stored at 4°C.

[0047] Then according to the above activity test method step 5 (preliminary screening of compound) and step 6 (IC of compound) 50 Determination of the value) described in the operation. Then take the logarithm of the concentration of 3-mercapto-2-methyl-N-phenylpropanamide as the abscissa and the residual activity of NDM-1 as the ordinate to draw a curve, as shown in FIG. 3 . Finally, according to the curve, using GraphPad Prismversion 5.0 software to calculate, the obtained IC 50 The value is 199.50±44.53 μM.

Embodiment 3

[0048] Example 3 Determination of NDM-1 activity inhibited by N-butyl-3-mercapto-2-methylpropionamide

[0049]

[0050] Dissolve the above-mentioned N-butyl-3-mercapto-2-methylpropionamide (4 mg) in 95% DMSO (228.1 μL) to prepare a solution with a concentration of 100 mM, and then place the solution in a 1.5 ml ep tube , stored at 4°C.

[0051] Then according to the above activity test method step 5 (preliminary screening of compound) and step 6 (IC of compound) 50 Determination of the value) described in the operation. Then take the logarithm of the concentration of N-butyl-3-mercapto-2-methylpropionamide as the abscissa and the residual activity of NDM-1 as the ordinate to draw a curve, as shown in FIG. 4 . Finally, according to the curve, using GraphPad Prismversion 5.0 software to calculate, the obtained IC 50 The value is 20.65±1.24 μM.

[0052] According to the above examples, it can be known that the compounds involved in the present invention have the effect of ...

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Abstract

The invention provides application of 3-mercaptopropionic acid amide compounds with the following general formula (I) in medicine which restrains the activity of multidrug-resistant bacteria through restraining the activity of NDM-1, wherein R1 is selected from a formula and R2 is selected from a C1-C4 alkyl group.

Description

technical field [0001] The present invention relates to the field of pharmacy, in particular to the use of 3-mercaptopropionamide 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 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/5375A61K31/167A61K31/16A61P31/04
CPCY02A50/30
Inventor 饶子和杨诚陈悦白翠改徐寅通李宁宁夏强
Owner TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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