Synthesis for biodegradable amphiphilic block copolymerization antibacterial peptoids, preparation method of antibacterial peptoid vesicles and applications of antibacterial peptoid vesicles
An amphiphilic block and antimicrobial peptide technology, which is applied in the direction of antibacterial drugs, drug combinations, peptide/protein components, etc., can solve the problems of high cost, complex extraction process of natural antimicrobial peptides, low yield, etc., and achieve low cost, Excellent broad-spectrum antibacterial performance, realizing the effect of industrial production
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[0084] A method for preparing the above-mentioned biodegradable amphiphilic block copolymerized antimicrobial peptides, which comprises the steps of:
[0085] (1), the preparation of the hydrophilic polypeptide segment containing amino protecting group:
[0086] (1-1), react the hydrophilic amino acid containing amino protecting group and triphosgene in an organic solvent to obtain the hydrophilic amino acid-N-carboxyl-α-amino acid anhydride monomer containing amino protecting group, which The structural formula is:
[0087]
[0088] Among them, R 1 Represents the hydrophilic group of a hydrophilic amino acid, and Z' represents an amino protecting group;
[0089] (1-2), the hydrophilic amino acid-N-carboxyl-α-amino acid anhydride monomer containing an amino protecting group and the initiator of the polymerization of the hydrophilic amino acid are dissolved in an organic solvent and reacted under vacuum to obtain Hydrophilic polypeptide chain segment containing amino prot...
Embodiment 1
[0147] The synthesis of biodegradable amphiphilic block-copolymerized antimicrobial peptides and the preparation method of antimicrobial peptide vesicles in this embodiment include the following steps:
[0148] (1) Add 20.000g (71.428mmol) benzyloxycarbonyl‐lysine and 10.598g (35.714mmol) triphosgene to 200mL tetrahydrofuran, the reaction temperature is 50°C, and react for 5h to obtain benzyloxycarbonyl‐lysine‐ N-carboxy-α-amino acid anhydride monomer, its structural formula is:
[0149]
[0150] (2) Dissolve 30.475mg (0.417mmol) isobutylamine (as an initiator), 3.000g (9.804mmol) benzyloxycarbonyl-lysine-N-carboxyl-α-amino acid anhydride monomer in 20mL dimethylmethylene In sulfone, vacuum reaction at 25°C for 12h to obtain poly(benzyloxycarbonyl-lysine), its structural formula is:
[0151]
[0152] (3) Add 2.121g (13.158mmol) tert-butoxycarbonyl (Boc)-aminoethanol (as an initiator), 30.00g (263.16mmol) caprolactone to 100mL toluene, and add 2 drops of stannous octoate...
Embodiment 2
[0171] The synthesis of biodegradable amphiphilic block-copolymerized antimicrobial peptides and the preparation method of antimicrobial peptide vesicles in this embodiment include the following steps:
[0172] (1) Add 10.000g (35.714mmol) benzyloxycarbonyl-lysine and 5.299g (17.857mmol) triphosgene to 100mL tetrahydrofuran, the reaction temperature is 50°C, and react for 5h to obtain benzyloxycarbonyl-lysine- N-carboxy-α-amino acid anhydride monomer, its structural formula is:
[0173]
[0174] (2) Dissolve 92.348mg (1.263mmol) isobutylamine (as an initiator), 5.000g (16.340mmol) benzyloxycarbonyl-lysine-N-carboxy-α-amino acid anhydride monomer in 20mL dimethylmethylene In sulfone, vacuum reaction at 20°C for 12h to obtain poly(benzyloxycarbonyl-lysine), its structural formula is:
[0175]
[0176] (3) Add 2.121g (13.158mmol) tert-butoxycarbonyl (Boc)-aminoethanol (as an initiator), 30.00g (263.16mmol) caprolactone to 100mL toluene, and add 2 drops of stannous octoate (a...
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