Aromatic phenol quaternary ammonium salt antibacterial peptide mimetic with antibacterial activity and preparation method thereof

A technology of antibacterial activity and antimicrobial peptide, applied in the field of medicinal chemistry, can solve the problems of easy degradation, weak selectivity, and high production cost of natural antimicrobial peptides, and achieve excellent antibacterial activity, high selectivity, and solve the problem of drug-resistant bacteria.
CN108558682BActive Publication Date: 2020-11-03ZHENGZHOU UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHENGZHOU UNIV
Publication Date
2020-11-03

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Abstract

The invention belongs to the technical field of medicine chemistry, and discloses an aromatic phenol antibacterial peptide simulant with anti-drug resistance activity and no obvious toxicity and a preparation method thereof. The target product is obtained through a reaction of 3 to 4 steps, and the main structure is shown below. Vitro antibacterial activity experiment proves that most of the compounds have good activity on gram-positive bacteria staphylococcus aureus and enterococcus faecalis, gram-negative bacteria large intestine angstrom bacillus and notrophomonas maltophilia, and shows that the compounds have excellent broad-spectrum antibacterial activity; meanwhile, the extracorporeal red blood cell hemolytic data shows that the toxicity is small, and the method has good selectivity.Part of the compounds shows excellent antibacterial activity in superbacteria including methicillin-resistant staphylococcus aureus (MRSA), NDM-1 and KPC-2 enzyme. Therefore, the compounds are expected to be used as a new antibacterial candidate drug.
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Description

technical field

[0001] The invention belongs to the technical field of medicinal chemistry, and discloses an aromatic phenol quaternary ammonium salt antibacterial peptide mimic with anti-drug-resistant bacteria activity and no obvious toxicity and a preparation method thereof. Background technique

[0002] The discovery and widespread use of antibiotics has indelible significance in the development of human civilization. According to different mechanisms, they are divided into aminoglycosides, tetracyclines, chloramphenicols, macrolides, lincomycetes, which affect bacterial protein synthesis. β-lactams that interfere with bacterial cell wall synthesis; polymyxins that damage bacterial cell membranes; sulfonamides and trimethoprim that interfere with folic acid metabolism; quinolones that affect nucleic acid metabolism, etc. However, due to the non-standard use of antibiotics, severe bacterial resistance problems have emerged, and even cross-resistance and multi-drug resista...

Claims

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