Synthesis and antibacterial activities of novel tyrocidine A glycosylated derivatives towards multidrug-resistant pathogens.
J Pept Sci
; 21(7): 586-92, 2015 Jul.
Article
em En
| MEDLINE
| ID: mdl-25900908
ABSTRACT
Glycosylation can have a multifaceted impact on the properties and functions of peptides and plays a critical role in interacting with or binding to the target molecules. Herein, based on the previously reported method for macrocyclic glycopeptide synthesis, two series of tyrocidine A glycosylated derivatives (1a-f and 2a-f) were synthesized and evaluated for their antibacterial activities to further study the structure and activity relationships (SAR). Biological studies showed that the synthetic glycosylated derivatives had good antibacterial activities towards methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus. SAR studies based on various glycans and linkages were used to enhance the biochemical profile, resulting in the identification of several potent antibiotics, such as 1f, with a great improved therapeutic index than tyrocidine A.
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Texto completo:
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tirocidina
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Farmacorresistência Bacteriana Múltipla
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Staphylococcus aureus Resistente à Meticilina
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Enterococos Resistentes à Vancomicina
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Antibacterianos
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article