Symmetrical lysine cation antibacterial peptide simulant with antibiotic synergistic activity and preparation method thereof

The invention belongs to the technical field of medicinal chemistry, and relates to a symmetrical lysine cation antibacterial peptide simulant with antibiotic synergistic activity and a preparation method of the symmetrical lysine cation antibacterial peptide simulant. An in-vitro antibacterial acti...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: HATAKAMI TAKASHI, ZHANG TINGTING, DU XIANGDANG, SHEN BOYUAN, LI SEN, ZHANG EN, KONG HONGTAO, LI SHIHONG, YAN DACHAO, YAO HONG, YAN TINGTING
Format: Patent
Sprache:chi ; eng
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The invention belongs to the technical field of medicinal chemistry, and relates to a symmetrical lysine cation antibacterial peptide simulant with antibiotic synergistic activity and a preparation method of the symmetrical lysine cation antibacterial peptide simulant. An in-vitro antibacterial activity experiment proves that the compound can enhance the activity of minocycline on gram-negative bacteria resistant to tetracycline antibiotics, such as carbapenem-resistant klebsiella pneumoniae, so that the MIC (minimal inhibitory concentration) of the minocycline is reduced by 8-128 times, and the compound 329 has better tetracycline antibiotic synergistic activity. A toxicity experiment result shows that the compound 329 hardly has hemolytic toxicity and has relatively low cytotoxicity. Mechanism research experiments find that the compound acts on bacterial cell membranes, permeability of outer membranes and inner membranes is increased, meanwhile, accumulation of minocycline in bacterial cells is promoted, an