Amphiphilic multi-block antibacterial peptide and preparation method and application thereof
A multi-block, antimicrobial peptide technology, applied in the direction of peptide preparation methods, antibacterial drugs, chemical instruments and methods, etc., can solve the problems of high cost, low yield, and complicated extraction process of natural antibacterial peptides, and achieve low cost, The effect of simple synthesis steps and excellent broad-spectrum antibacterial properties
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[0077]
[0078] The preparation method of the amphiphilic multi-block antimicrobial peptide comprises the following steps:
[0079] (1), the preparation of hydrophobic polypeptide block:
[0080] (1-1), react the hydrophobic amino acid containing amino protecting group, N,N'-dicyclohexylcarbodiimide and N-hydroxysuccinimide in organic solvent to obtain amino protecting group-containing amino acid Hydrophobic amino acid activated ester monomer, its structural formula is:
[0081]
[0082] where R 1 Represents the hydrophobic group of the hydrophobic amino acid, and A' represents the amino protecting group of the hydrophobic amino acid;
[0083] (1-2), dissolving the hydrophobic amino acid activated ester monomer containing an amino protecting group and the hydrophobic molecular segment of the polymerization initiation in an organic solvent and reacting to obtain a first reactant containing an amino protecting group, which The structural formula is:
[0084]
[0085]...
Embodiment 1
[0131] The amphiphilic multi-block antimicrobial peptide K of this example 3 F 6 K 3 The preparation method comprises the following steps:
[0132] (1) 10.0 g (37.7 mmol) of N-α-tert-butoxycarbonyl-L-phenylalanine was added to 50 mL of tetrahydrofuran, and placed in an ice-water bath. 7.8 g of DCC and 4.8 g of HOSu (1.1 times the amount of phenylalanine species) were dissolved in 20 mL of tetrahydrofuran, and then added dropwise to the tetrahydrofuran solution of phenylalanine over 30 minutes. The ice-water bath was removed, and the reaction was stirred at 25 °C for 8 h; after the reaction was completed, suction filtration was performed, the solid was discarded, and the clarified filtrate was the Boc-protected phenylalanine activated ester monomer, and its structural formula was:
[0133]
[0134] Wherein, Boc represents the amino protecting group of phenylalanine;
[0135] (2) Dissolve 2.192g (0.019mol) of hexanediamine in 10mL of tetrahydrofuran, slowly dropwise add 1...
Embodiment 2
[0151] The amphiphilic multi-block antimicrobial peptide K of this example 4 F 8 K 4 The preparation method comprises the following steps:
[0152] (1) 10.0 g (25.8 mmol) of N-α-fluorenylmethoxycarbonyl-L-phenylalanine was added to 50 mL of tetrahydrofuran, and placed in an ice-water bath. 5.3 g of DCC and 3.3 g of HOSu (1.1 times the amount of phenylalanine species) were dissolved in 20 mL of tetrahydrofuran, and then added dropwise to a solution of phenylalanine in tetrahydrofuran over 30 minutes. The ice-water bath was removed, and the reaction was stirred at 25 °C for 8 h; after the reaction was completed, suction filtration was performed, the solid was discarded, and the clarified filtrate was the Fmoc-protected phenylalanine activated ester monomer, and its structural formula was:
[0153]
[0154] Wherein, Fmoc represents the amino protecting group of phenylalanine;
[0155] (2) Dissolve 1.499g (0.013mol) of hexanediamine in 10mL of tetrahydrofuran, slowly dropwi...
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