Synthesis of low-hemolytic antimicrobial dehydropeptides based on gramicidin s.
J Med Chem
; 49(26): 7592-5, 2006 Dec 28.
Article
em En
| MEDLINE
| ID: mdl-17181140
ABSTRACT
The synthesis and biological activity of a novel cyclic beta-sheet-type antimicrobial dehydropeptide based on gramicidin S (GS) is described. The GS analogue, containing two (Z)-(beta-3-pyridyl)-alpha,beta-dehydroalanine (DeltaZ3Pal) residues at the 4 and 4' positions (2), was synthesized by solution-phase methodologies using Boc-Leu-DeltaZ3Pal azlactone. Analogue 2 exhibited high antimicrobial activity against Gram-positive bacteria and had much lower hemolytic activity than wild-type GS and the corresponding (Z)-alpha,beta-dehydrophenylalanine (DeltaZPhe) analogue (1).
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Base de dados:
MEDLINE
Assunto principal:
Alanina
/
Bactérias Gram-Positivas
/
Gramicidina
/
Hemólise
/
Antibacterianos
Idioma:
En
Ano de publicação:
2006
Tipo de documento:
Article