Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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

A technology for indolin diketone thiosemicarbazone compounds, which is applied in the directions of organic active ingredients, antibacterial drugs, pharmaceutical formulations, etc., can solve the problems such as the application of indolin diketone thiosemicarbazone compounds that have not yet been seen , to achieve good drug application prospects, alleviate drug resistance, and improve the effect of efficacy

Inactive Publication Date: 2013-10-16
TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE +1
View PDF5 Cites 0 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com