Antifungal activity of 2I+/-,3I2-functionalized steroids stereoselectively increases with the addition of oligosaccharides

Invasive fungal infections pose a significant problem to the immune-compromised. Moreover, increased resistance to common antifungals requires development of novel compounds that can be used to treat invasive fungal infections. Naturally occurring steroidal glycosides have been shown to possess a ra...

Full description

Saved in:
Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 21; no. 24; pp. 7379 - 7386
Main Authors Cammarata, Amy, Upadhyay, Sunil Kumar, Jursic, Branko S, Neumann, Donna M
Format Journal Article
LanguageEnglish
Published 15.12.2011
Subjects
Antifungal activity
Antimicrobial agents
Data processing
glycosides
Infection
Mammalian cells
oligosaccharides
Pathogens
Steroid hormones
Toxicity
Online AccessGet full text

Cover

More Information
Summary:Invasive fungal infections pose a significant problem to the immune-compromised. Moreover, increased resistance to common antifungals requires development of novel compounds that can be used to treat invasive fungal infections. Naturally occurring steroidal glycosides have been shown to possess a range of functional antimicrobial properties, but synthetic methodology for their development hinders thorough exploration of this class of molecules and the structural components required for broad spectrum antifungal activity. In this report, we outline a novel approach to the synthesis of glycoside-linked functionalized 2I+/-,3I2-cholestane and spirostane molecules and present data from in vitro screenings of the antifungal activities against human fungal pathogens and as well as mammalian cell toxicity of these derivatives.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
content type line 23
ObjectType-Feature-1
ISSN:0960-894X
DOI:10.1016/j.bmcl.2011.10.015