http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2018108154-A1

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publicationDate 2018-06-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2018108154-A1
titleOfInvention Polymyxin derivative, preparation method and application thereof
abstract 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 "super bacteria" which carries the NDM-1 gene.
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