Novel dendrimeric lipopeptides with antifungal activity
| Autor: | Aleksandra Rajnisz, Zofia Urbanczyk-Lipkowska, Jolanta Solecka, Sławomir Milewski, Izabela Łącka, Jolanta Janiszewska, Marta Sowinska |
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| Rok vydání: | 2011 |
| Předmět: |
Dendrimers
Antifungal Agents Erythrocytes Clinical Biochemistry Pharmaceutical Science Microbial Sensitivity Tests Biochemistry Minimum inhibitory concentration Lipopeptides Dendrimer Cations Drug Discovery Potency Cationic Lipopeptides Humans Molecular Biology Candida ATP synthase biology Bacteria Molecular Structure Chemistry Organic Chemistry Antimicrobial biology.organism_classification In vitro Glucosyltransferases Drug Design biology.protein Molecular Medicine |
| Zdroj: | Bioorganicmedicinal chemistry letters. 22(3) |
| ISSN: | 1464-3405 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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