Dialkyl cationic amphiphilic antibacterial peptide analogue with antibacterial activity and preparation method thereof

A technology of dialkyl cation and antibacterial activity is applied in the field of dialkyl cation amphiphilic antibacterial peptide mimics and their preparation, and achieves the effects of good bacteriostatic effect, broad antibacterial spectrum and remarkable selectivity

Active Publication Date: 2017-08-01
ZHENGZHOU UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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  • Dialkyl cationic amphiphilic antibacterial peptide analogue with antibacterial activity and preparation method thereof
  • Dialkyl cationic amphiphilic antibacterial peptide analogue with antibacterial activity and preparation method thereof
  • Dialkyl cationic amphiphilic antibacterial peptide analogue with antibacterial activity and preparation method thereof

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Embodiment 1

[0062] The preparation of embodiment 1 compound 4a-4r

[0063] (1) Synthesis of compounds (1d, 1f, 1h):

[0064] Compounds (1a-1c, 1e, 1g) are commercially available. Compounds (1d, 1f, 1h) were synthesized by the traditional method: add solvent DMF (N,N-dimethylformamide) to a flask containing a mixture of n-alkylamine and brominated alkanes, and then add anhydrous carbonic acid Potassium (n-alkylamine: bromoalkane: anhydrous potassium carbonate = 1:1:1), then stirred at 80°C for 12h. Add chloroform and water after the reaction to extract, separate the organic layer, extract three times with chloroform, wash twice with water, wash once with saturated brine, dry over anhydrous magnesium sulfate, filter and evaporate to dryness, and the crude product is separated by column chromatography (petroleum ether : ethyl acetate: triethylamine=10:1:0.05).

[0065] (2) Synthesis of compound (2a-2i):

[0066] Synthesis of compound (2a, 2e-2i): 5g of amino acids (L-lysine, L-alanine, L...

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Abstract

The invention belongs to the field of medicinal chemistry, and discloses a dialkyl cationic amphiphilic antibacterial peptide analogue with antibacterial activity and a synthesis method thereof. Through four-step reaction, a target product can be simply and fast obtained. A major structure is shown as the accompanying drawing. In-vitro antibacterial activity experiments prove that the most compounds in the series show good antibacterial effects on staphylococcus aureus and escherichia coli; partial compounds show excellent antibacterial activity on super bacteria including MRSA (methicillin-resistance staphylococcus aureus), VRE (vancomycin-resistant enterococcus) and CRE (carbapenemase enterobacteriaceae). In-vitro red cell toxicity experiments also show the series of compounds have low red cell toxicity, so that the series of compounds are hopeful to be used as novel antibacterial candidate medicine. The formulas are shown in the description.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and discloses a dialkyl cationic amphiphilic antibacterial peptide mimetic with antibacterial activity and a preparation method thereof. Background technique [0002] Antimicrobial peptides are a kind of polypeptide substances that widely exist in natural organisms. As the first line of defense of biological organisms, they can resist the invasion of pathogens. Antibacterial peptides have various biological activities such as anti-bacteria, fungi, viruses, and inhibiting and killing cancer cells. Not easy to develop drug resistance. With the emergence of more and more antibiotic-resistant microorganisms, antimicrobial peptides have good application prospects in the pharmaceutical industry and food additives. These characteristics make antimicrobial peptides the most promising alternative to traditional antibiotics. Therefore, it is imminent to synthesize antimicrobial peptide compoun...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C231/12C07C237/06C07C279/14C07C237/20C07C277/08A61P31/00
CPCY02P20/55C07C237/06C07C237/20C07C279/14
Inventor 张恩秦上尚白鹏燕王铭铭刘琴殷海洋张勇杰王上王亚娜崔得运化永刚楚文超刘宏民
Owner ZHENGZHOU UNIV
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