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

Levo-fluoroquinolone C3 bisazole methyl sulfide, preparation method and application thereof

A technology of levofluoroquinolones and fluoroquinolones, which is applied in the field of medicine, can solve the problems that the study of electron isosteres has not been reported, and achieve the effects of strong in vitro cytotoxicity and strong anti-tumor activity

Inactive Publication Date: 2012-03-28
河南省健康伟业生物医药研究股份有限公司
View PDF6 Cites 23 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, although there are a large number of synthetic reports on azole compounds, the research on the isosteres of the C-3 carboxyl group of levofloxacin has not been reported yet.

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
  • Levo-fluoroquinolone C3 bisazole methyl sulfide, preparation method and application thereof
  • Levo-fluoroquinolone C3 bisazole methyl sulfide, preparation method and application thereof
  • Levo-fluoroquinolone C3 bisazole methyl sulfide, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] (S)-8,1-[1,2-(oxypropyl)]-6-fluoro-7-(4-methylpiperazin-1-yl)-3-[5-(5-phenyl- 1,3,4-oxadiazol-2-methylthio)-1,3,4-oxadiazol-2-yl]-4(1H)-quinolinone, the structural formula is:

[0043]

Embodiment 2

[0045] (S)-8,1-[1,2-(oxypropyl)]-6-fluoro-7-(4-methylpiperazin-1-yl)-3-[5-(5-p-methoxy Phenyl-1,3,4-oxadiazol-2-methylthio)-1,3,4-oxadiazol-2-yl]-4(1H)-quinolinone, the structural formula is:

[0046]

Embodiment 3

[0048] (S)-8,1-[1,2-(oxypropyl)]-6-fluoro-7-(4-methylpiperazin-1-yl)-3-[5-(5-p-tolyl -1,3,4-oxadiazol-2-methylthio)-1,3,4-oxadiazol-2-yl]-4(1H)-quinolinone, the structural formula is:

[0049]

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 belongs to the technical field of medicine, and in particular discloses a levo-fluoroquinolone C3 bisazole methyl sulfide, a preparation method and application thereof in the field of pharmacy. The chemical structural formula of the levo-fluoroquinolone C3 bisazole methyl sulfide is shown as a general formula I, wherein in the general formula I, X is selected from any one of O, S and -NH; and Ar is selected from any one of phenyl, substituent-containing phenyl and heterocyclic aromatic hydrocarbon. The levo-fluoroquinolone C3 bisazole methyl sulfide has strong in vitro cytotoxin effect on experimental leukemia cancer cell strains, has strong anti-tumor activity, and can be mixed with a human acceptable acid salt or a medicinal carrier to prepare an anti-tumor medicament.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to levofluoroquinolone C3 bisazole methide, and also relates to a preparation method of levofluoroquinolone C3 bisazole methide and its application in the field of pharmacy. Background technique [0002] Fluoroquinolones (FQ) are clinical antibacterial drugs developed in the 1980s, represented by norfloxacin. Based on the similar function of its target topoisomerase (TOPO) and mammalian TOPO, it is a new research direction to transform antibacterial FQ into antitumor FQ. Although anti-tumor FQ compounds including bicyclic quinolones, tricyclic quinolones, tetracyclic quinolones, chiral quinolones, flavonoids and other anti-tumor FQ compounds have been designed and synthesized, at present, these compounds have toxicity and activity in parallel to varying degrees, and poor solubility in vivo Lead to common problems such as low bioavailability and easy metabolic inactivation in vivo ...

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 Applications(China)
IPC IPC(8): C07D498/06A61K31/5383A61P35/00
Inventor 胡国强叶乾堂于振艳陈蕴刘浩李建勋康建党黄福生
Owner 河南省健康伟业生物医药研究股份有限公司
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