Synthesis and antibacterial studies of teixobactin analogues with non-isostere substitution of enduracididine.
Bioorg Med Chem
; 26(5): 1062-1068, 2018 03 01.
Article
em En
| MEDLINE
| ID: mdl-29398444
ABSTRACT
Teixobactin is a structurally and mechanistically novel antimicrobial peptide with potent activities against Gram-positive pathogens. It contains l-allo-enduracididine (End) residue which is not readily accessible. In this report, we have used convergent Ser Ligation as the key step to prepare a series of teixobactin analogues with End being substituted with its non-isostere moieties. Among these analogues, compounds T16, T27 and T29 exhibited the best antimicrobial activities against different Gram-positive bacteria with MICs ranging from 0.25 to 1.0⯵M. Structure-activity relationship is also established for further development of more promising teixobactin analogues.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirrolidinas
/
Depsipeptídeos
/
Antibacterianos
Idioma:
En
Revista:
Bioorg Med Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2018
Tipo de documento:
Article