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...

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Hauptverfasser: HATAKAMI TAKASHI, ZHANG TINGTING, DU XIANGDANG, SHEN BOYUAN, LI SEN, ZHANG EN, KONG HONGTAO, LI SHIHONG, YAN DACHAO, YAO HONG, YAN TINGTING
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creator HATAKAMI TAKASHI
ZHANG TINGTING
DU XIANGDANG
SHEN BOYUAN
LI SEN
ZHANG EN
KONG HONGTAO
LI SHIHONG
YAN DACHAO
YAO HONG
YAN TINGTING
description 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
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subjects ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title Symmetrical lysine cation antibacterial peptide simulant with antibiotic synergistic activity and preparation method thereof
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