Document Detail


Novel dendrimeric lipopeptides with antifungal activity.
MedLine Citation:
PMID:  22230049     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A series of new cationic lipopeptides containing branched, amphiphilic polar head derived from (Lys)Lys(Lys) dendron and C(8) or C(12) chain at C-end were designed, synthesized and characterized. Antimicrobial in vitro activity expressed as minimal inhibitory concentration (MIC) was evaluated against Gram-positive and Gram-negative bacteria and yeasts from the Candida genus. A significant enhancement of antimicrobial potency along with increased selectivity against Candida reference strains was detected for derivatives with the C(12) residue. Several compounds were characterized by a low hemotoxicity. The antifungal activity of branched lipopeptides is multimodal and concentration dependent. Several compounds, studied in detail, induced potassium leakage from fungal cells, caused morphological alterations of fungal cells and inhibited activity of candidal β(1,3)-glucan synthase.
Authors:
Jolanta Janiszewska; Marta Sowińska; Aleksandra Rajnisz; Jolanta Solecka; Izabela Łącka; Sławomir Milewski; Zofia Urbańczyk-Lipkowska
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2011-12-17
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  22     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2012 Feb 
Date Detail:
Created Date:  2012-01-27     Completed Date:  2012-04-27     Revised Date:  2012-09-27    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  1388-93     Citation Subset:  IM    
Copyright Information:
Copyright © 2011 Elsevier Ltd. All rights reserved.
Affiliation:
Institute of Industrial Research, L. Rydygiera 8, 01-793 Warsaw, Poland.
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MeSH Terms
Descriptor/Qualifier:
Antifungal Agents / chemical synthesis,  chemistry*,  pharmacology*
Bacteria / drug effects
Candida / drug effects*,  enzymology,  ultrastructure
Cations
Dendrimers / chemical synthesis,  chemistry*,  pharmacology*
Drug Design
Erythrocytes / drug effects
Glucosyltransferases / antagonists & inhibitors
Humans
Lipopeptides / chemical synthesis,  chemistry*,  pharmacology*
Microbial Sensitivity Tests
Molecular Structure
Chemical
Reg. No./Substance:
0/Antifungal Agents; 0/Cations; 0/Dendrimers; 0/Lipopeptides; EC 2.4.1.-/Glucosyltransferases; EC 2.4.1.-/glucan synthase
Comments/Corrections
Erratum In:
Bioorg Med Chem Lett. 2012 Aug 15;22(16):5330

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