A kind of method for preparing peregrine

A liquid-phase and solid-phase synthesis technology, applied in the preparation methods of peptides, chemical instruments and methods, animal/human peptides, etc., can solve the problems of unsuitability for large-scale production, low purity and yield, and long synthesis cycle. and other problems, to achieve the effect of low cost, low cost and short synthesis cycle
CN104356221BActive Publication Date: 2018-06-26上海飞腾医药科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
上海飞腾医药科技有限公司
Publication Date
2018-06-26

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Abstract

The invention relates to the technical field of polypeptide synthesis, in particular to a preparation method of pexiganan. The preparation method comprises the following specific steps: A) synthesizing a dipeptide fragment FmoC-Lys (BoC)-Lys (BoC)-OH by a liquid phase method; B) by a solid-phase synthesis method, with amino resin as starting resin, sequentially coupling amino acids with FmoC protections at N terminals and side chain protections according to a peptide sequence of a main chain of the pexiganan, wherein the amino acids at 7 and 8 positions, the amino acids 10 and 11 positions and the amino acids at 21 and 22 positions are coupled by the dipeptide fragment FmoC-Lys (BoC)-Lys (BoC)-OH; C) cracking, purifying and freeze-drying peptide resin to obtain the pexiganan. The invention provides a synthesis process of the pexiganan, which is high in synthesis efficiency and low in cost, can avoid deleted peptide impurities caused by incomplete coupling of two lysines and is suitable for mass production.
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Description

technical field

[0001] The invention relates to a method for preparing polypeptide antibiotics, in particular to a method for preparing pexicanan. Background technique

[0002] Pexiganan, English name: pexiganan, is a linear polypeptide containing 22 amino acids, the peptide sequence is:

[0003]

[0004] Percycanan is a product jointly developed by GlaxoSmithKline and Genaera (formerly Magainin Pharmaceuticals). It is used as a broad-spectrum topical antimicrobial agent in the treatment of infected diabetic foot ulcers. Percycanan was originally isolated from the abdominal skin of Xenopus laevis. It is a polypeptide antibacterial drug of animal origin. It is a member of the polypeptide antibiotic family magainin, and it is also the second new antibiotic family in the past 20 years. It can effectively Against more than 3,000 isolates, including bacteria (gram-negative, gram-positive and anaerobic), amoebas, fungi and parasites. The mechanism of action of peciganan is d...

Claims

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