Pegylated polypeptide prodrug synthesis technology based on photo-regulation, and purpose of pegylated polypeptide prodrug synthesis technology for preparing antimicrobial drug
The invention belongs to the field of medicine synthesis, and particularly relates to a synthesis technology for photosensitive compounds cGS-mPEG and cIN-mPEG, and a purpose of the synthesis technology for preparing an antimicrobial drug. 4'-hydroxyl-3'-methoxyacetophenone is taken as a s...
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Main Authors | , , , , |
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Format | Patent |
Language | Chinese English |
Published |
03.04.2020
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Subjects | |
Online Access | Get full text |
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Summary: | The invention belongs to the field of medicine synthesis, and particularly relates to a synthesis technology for photosensitive compounds cGS-mPEG and cIN-mPEG, and a purpose of the synthesis technology for preparing an antimicrobial drug. 4'-hydroxyl-3'-methoxyacetophenone is taken as a starting material to prepare a photosensitive radical (2-nitrobenzyl, NB), then, the photosensitive radical isintroduced to a side chain amino position to pre-prepare photosensitive ornithine and lysine; and through solid phase peptide synthesis, antimicrobial peptides Gramicidin S (GS) and Indolicidin (IN) containing the photosensitive radical are prepared. Connection of the peptide and monomethoxy polyethyleneglycol (mPEG) is realized through a strategy of (click reaction). The mPEG is substituted through azides, and then, the click reaction is carried out with the alkyne of the photosensitive radical so as to connect the peptide with the mPEG to prepare cGS-mPEG and ccIN-mPEG. Before the category of compounds is not irradi |
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Bibliography: | Application Number: CN202010029395 |