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De novo cyclic pseudopeptides containing aza-β3-amino acids exhibiting antimicrobial activities.
MedLine Citation:
PMID:  23148564     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
de novo cyclic pseudopeptides composed of α-amino and aza-β3-amino acids were designed with the aim to obtain potential new antimicrobial agents. Antimicrobial Cyclic PseudoPeptides (ACPPs) are based on the properties of Antimicrobial Peptides (AMPs), so they are cationic and amphiphilic. Aza-β3-amino acids enhance the in vivo half-life of these compounds and offer the possibility to incorporate a large variety of side chains. Most of the thirteen ACPPs exert antimicrobial activities in rich media with broad-spectrum of antibacterial activities. Selectivity for bacterial over mammalian cells was determined by testing the hemolytic activities of ACPPs against sheep Red Blood Cells (sRBC). We examined the ratio of cationic to hydrophobic residues as well as the type of hydrophobic side chains essential for biological activity of this class of ACPPs. These results will be useful for designing potential candidates for a therapeutic application.
Authors:
Mathieu Laurencin; Amor Mosbah; Yannick Fleury; Michèle Baudy-Floc'h
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-11-13
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  -     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2012 Nov 
Date Detail:
Created Date:  2012-11-14     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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