Novel effective antibacterial small-molecules against Staphylococcus and Enterococcus strains.
Future Med Chem
; 12(13): 1205-1211, 2020 07.
Article
em En
| MEDLINE
| ID: mdl-32515228
ABSTRACT
Background:
Resistance developments against established antibiotics are an emerging problem for antibacterial therapies. Novel antibiotics are urgently needed. Materials &methods:
We developed novel small-molecule antibacterials which are easily accessible in a simple one-pot synthesis. The central cyclopentaindole core is substituted with two indole residues. Various indole and cyclopentane substituents have been introduced. Additionally, first indole substituted propene compounds as ring-open variants of the cyclopentaindoles have been yielded and evaluated as antibacterials against Staphylococcus aureus and Enterococcus strains.Results:
Most effective compounds have been those with a bromo cyclopentane and a chloro indole substitution. First lead compounds were identified with promising activities similar to that observed in vitro for last resort antibiotics, so that the novel compounds enriche the pool of perspective small-molecule antibacterial drug candidates.Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Staphylococcus
/
Enterococcus
/
Bibliotecas de Moléculas Pequenas
/
Hidrocarbonetos Bromados
/
Hidrocarbonetos Iodados
/
Antibacterianos
Idioma:
En
Revista:
Future Med Chem
Ano de publicação:
2020
Tipo de documento:
Article
País de afiliação:
Alemanha