Synthesis and Evaluation of Troponoids as a New Class of Antibiotics.
ACS Omega
; 3(11): 15125-15133, 2018 Nov 30.
Article
en En
| MEDLINE
| ID: mdl-30533576
ABSTRACT
Novel antibiotics are urgently needed. The troponoids [tropones, tropolones, and α-hydroxytropolones (α-HT)] can have anti-bacterial activity. We synthesized or purchased 92 troponoids and evaluated their antibacterial activities against Staphylococcus aureus, Escherichia coli, Acinetobacter baumannii, and Pseudomonas aeruginosa. Preliminary hits were assessed for minimum inhibitory concentrations (MIC80) and cytotoxicity (CC50) against human hepatoma cells. Sixteen troponoids inhibited S. aureus/E. coli/A. baumannii growth by ≥80% growth at <30 µM with CC50 values >50 µM. Two selected tropolones (63 and 285) inhibited 18 methicillin-resistant S. aureus (MRSA) strains with similar MIC80 values as against a reference strain. Two selected thiotropolones (284 and 363) inhibited multidrug-resistant (MDR) E. coli with MIC80 ≤30 µM. One α-HT (261) inhibited MDR-A. baumannii with MIC80 ≤30 µM. This study opens new avenues for development of novel troponoid antibiotics to address the critical need to combat MDR bacterial infections.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Idioma:
En
Revista:
ACS Omega
Año:
2018
Tipo del documento:
Article
País de afiliación:
Estados Unidos