Synthesis and evaluation of analogues of the glycinocin family of calcium-dependent antibiotics.
Org Biomol Chem
; 16(29): 5310-5320, 2018 07 25.
Article
em En
| MEDLINE
| ID: mdl-29993080
ABSTRACT
The glycinocins are a class of calcium-dependent, acidic cyclolipopeptide antibiotics that are structurally related to the clinically approved antibiotic daptomycin. In this article, we describe the synthesis of a small library of glycinocin analogues that differ by variation in the exocyclic fatty acyl substituent. The glycinocin analogues were screened against a panel of Gram-positive bacteria (as well as Gram-negative P. aeruginosa). These analogues exhibited similar calcium-dependent activity to the parent natural products against Gram-positive bacteria but showed no activity against P. aeruginosa. The length of the fatty acid was shown to be important for optimal biological activity, while the hybridisation at the α,ß position and branching within the fatty acyl chain had only subtle effects on activity.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Peptídeos
/
Antibacterianos
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article