Design, synthesis and biological evaluation of novel indole-piperazine derivatives as antibacterial agents.
Bioorg Med Chem Lett
; 89: 129320, 2023 06 01.
Article
em En
| MEDLINE
| ID: mdl-37156392
Herein, a series of novel indole-piperazine derivatives were synthesized. Bioassay results showed the title compounds exhibited moderate to good bacteriostatic efficacy against the test Gram-positive bacteria and Gram-negative bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). Among theses compounds, three remarkable compounds 8f, 9a, and 9h exhibited superior in vitro antibacterial profiles for anti- S. aureus and anti-MRSA to that of gentamicin. Hit compound 9a manifested a rapid bactericidal kinetic effect on MRSA, with no resistance observed after 19 days of sequential passaging. And 8 µg/mL of compound 9a displayed considerable post antibacterial effects to that of ciprofloxacin at the concentration of 2 µg/mL. Cytotoxic and ADMET studies indicated, to some extent, compounds 8f, 9a, and 9h were up to the standard for antibacterial drugs. These results suggest that indole/piperazine derivatives based on the title compounds can serve as a new scaffold for antimicrobial development.
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Base de dados:
MEDLINE
Assunto principal:
Staphylococcus aureus Resistente à Meticilina
/
Antibacterianos
Idioma:
En
Ano de publicação:
2023
Tipo de documento:
Article