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

Secondary 8-hydroxyquinoline-7-carboxamide derivatives for use as antifungal agents

一种抗真菌剂、羧酰胺的技术，应用在用作抗真菌剂的仲8-羟基喹啉-7-羧酰胺衍生物领域，能够解决窄作用范围、药物不令人满意、药代动力学特性严重等问题

Inactive Publication Date: 2015-12-23
POLICHEM SA
View PDF9 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Unfortunately, the drugs available in practice are unsatisfactory due to their narrow action spectrum, pharmacokinetic profile and severe side effects

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
  • Secondary 8-hydroxyquinoline-7-carboxamide derivatives for use as antifungal agents
  • Secondary 8-hydroxyquinoline-7-carboxamide derivatives for use as antifungal agents
  • Secondary 8-hydroxyquinoline-7-carboxamide derivatives for use as antifungal agents

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0289]

[0290] 8-Hydroxy-N-(thiophen-2-ylmethyl)quinoline-7-carboxamide

[0291] A mixture of 8-hydroxyquinoline-7-carboxylic acid (100 mg, 0.53 mmol) and bis(1H-imidazol-1-yl)methanone (86 mg, 0.53 mmol) in THF (8 mL) was heated to 45 °C under nitrogen. ℃ overnight. The reaction mixture was cooled to room temperature and thiophen-2-ylmethylamine (30 mg, 0.26 mmol) was added. The resulting mixture was stirred at room temperature for 24 hours. Additional thiophen-2-ylmethylamine (15 mg, 0.13 mmol) was added and the reaction mixture was stirred at room temperature for 60 hours. with H 2 O quenched the reaction mixture and evaporated THF to dryness. A saturated solution of sodium bicarbonate was added to the aqueous phase and extracted twice with DCM. by Na 2 SO 4 The separated organics were dried, filtered and concentrated under reduced pressure. The residue was purified by SPE-SI cartridge (2 g, DCM to DCM:MeOH 99:1 ) to provide the title compound (40 mg, 0.14 mmol)...

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 present invention provides secondary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopulariopsis Brevicaulis. These compounds are active against Candida species such as Candida Albicans and Candida Glabrata.

Description

[0001] This application is a divisional application of the application dated December 28, 2010, the application number is 201080059739.X, and the title of the invention is "secondary 8-hydroxyquinoline-7-carboxamide derivatives used as antifungal agents" . technical field [0002] The present invention provides secondary 8-hydroxyquinoline-7-carboxamide derivatives and pharmaceutically acceptable salts thereof useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopulariopsis Brevicaulis. These compounds are effective against Candida species such as Candida Albicans and Candida Glabrata. Background technique [0003] Pathogenic fungi can be divided into two groups: fungi capable of causing disease in normal subjects and less invasive fungi capable of producing disease only in severely diseased hosts. The incidence of invasive opportunistic fungal infections and the associated m...

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): A61K31/47A61K31/4709A61P31/10
CPCC07D215/48C07D405/12C07D409/12C07D413/12C07D417/12C07D401/12A61P31/00A61P31/10
Inventor 斯特凡尼娅·加利亚尔迪西蒙·德尔索尔多F·马兰德M·勒戈拉
Owner POLICHEM SA
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