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Application of isatin thiosemicarbazone compound in inhibition of NDM-1 activity

A technology of indolin diketide thiosemicarbazide and NDM-1 is applied in the directions of organic active ingredients, medical preparations containing active ingredients, antibacterial drugs, etc. problems such as the application of thiourea compounds, to achieve good drug application prospects, eliminate hydrolysis, and improve the effect of curative effect

Inactive Publication Date: 2012-08-08
TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The application of indolindiketone thiosemicarbazone compounds in inhibiting NDM-1 activity has not been seen so far

Method used

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  • Application of isatin thiosemicarbazone compound in inhibition of NDM-1 activity
  • Application of isatin thiosemicarbazone compound in inhibition of NDM-1 activity
  • Application of isatin thiosemicarbazone compound in inhibition of NDM-1 activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Compound 1

[0040]

[0041] Mix 7-iodoindolindione (2.7g, 10mmol) and phenylthiosemicarbazide (1.7g, 10mmol) with 5mL of acetic acid, reflux in 50mL of ethanol-water (5:1) solution for 6h, and then cool to At room temperature, recrystallization from ethanol solution gave 2.7 g of the title compound with a yield of 65%.

Embodiment 2

[0042] Example 2: Compound 2

[0043]

[0044] The 7-iodoindolindione in Example 1 was replaced with 7-bromoindolindione, and the compound was prepared by the same preparation method as in Example 1.

Embodiment 3

[0045] Example 3: Compound 3

[0046]

[0047] The 7-iodoindolindione in Example 1 was replaced by 7-methylindolindione, and the compound was prepared by the same preparation method as in Example 1.

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PUM

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Abstract

The invention provides application of isatin thiosemicarbazone compound with the following general formula (I) in preparing medicament for inhibiting activity of NDM-1. In the formula (I), R1 is selected from the group consisting of hydrogen and C5-C10 aralkyl; R2 is selected from the group consisting of hydrogen, C1-C4 alkyl and halogen; and R3 is selected from the group consisting of hydrogen and C1-C4 alkyl. The compound can significantly inhibit the activity of NDM-1.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to the application of indolindione thiosemicarbazone compounds. Background technique [0002] In August 2010, Walsh TR et al. (Lancet Infect Dis.2010, 10(9), 597-602) reported a case of drug resistance to all β-lactam antibiotics, insensitivity to ciprofloxacin, and only In the case of mycocin sensitivity, in-depth research found that it carried a new type of metallo-β-lactamase encoded by Klebsiella pneumoniae, and named this enzyme New Delhi metallo β-lactamase (NDM-1, New Delhi metallo-β-lactamase-1). [0003] The main bacteria carrying NDM-1 are Escherichia coli and Klebsiella pneumoniae, other bacteria include Enterobacter cloacae, Proteus species, Citrobacter freundii (Citrobacter freundii), Klebsiella oxytoca, Morganella morganii, Providencia Ewing, etc. These bacteria mainly cause infections of the urinary tract, bloodstream, wounds, lungs, and catheters. In less than ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/404A61P31/04
Inventor 郭宇王建国杨诚王伟民王静商建丽饶子和李正名
Owner TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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