CHINESE ACADEMY OF MEDICAL SCIENCES;INSTITUTE OF MEDICINAL BIOTECHNOLOGY
发明人:
ALONG CUI,ZHUORONG LI,JIE JIN,YAN GAO,XINXIN HU,XUEFU YOU,YANG CHEN,QIYANG HE
申请号：
US16468997
公开号：
US20190315806A1
申请日:
2017.12.15
申请国别(地区):
US
年份:
2019
代理人:
摘要：
Provided are a polymyxin derivative having a general formula I structure, and a preparation method and an application thereof. The method for preparing the polymyxin derivative comprises the following steps: (1) an Fmoc-AA-OP side chain free amino group of a protected basic amino acid reacting with a halogenated resin to obtain an Fmoc-AA-OP-resin； (2) the Fmoc-AA-OP-resin being coupled one by one to obtain a linear peptide-resin； (3) the linear peptide-resin selectively removing a protective group, and carrying out solid-phase cyclization to obtain a cyclic peptide-resin； (4) the cyclic peptide-resin undergoing acidic hydrolysis and ether precipitation to obtain a crude product of a cyclic polypeptide； (5) the crude product being purified and/or salt transferred and lyophilized to obtain a pure product of the cyclic polypeptide. The polymyxin derivative may be used for preparing an antibacterial drug, and used in particular for preparing an antibacterial drug having an expanded antibacterial spectrum, improved antibacterial activity and reduced renal toxicity, comprising preparing an antibacterial drug against a “superbugs” which carries the NDM-1 gene.
