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Glycosylated glycopeptide antibiotic derivative

一种糖肽、化合物的技术，应用在抗菌素、抗菌素、肽等方向，能够解决没有记载氨基化学修饰化合物等问题

Inactive Publication Date: 2011-01-26
SHIONOGI & CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, Non-Patent Document 11 (Angewandte Chemie, International Edition (2003), 42(38), 4657-4660) describes that -CH is bonded to galactose at the end of the sugar chain 2 NH 2 vancomycin derivatives, but there is no record of compounds that further chemically modify the amino group

Method used

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  • Glycosylated glycopeptide antibiotic derivative
  • Glycosylated glycopeptide antibiotic derivative
  • Glycosylated glycopeptide antibiotic derivative

Examples

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preparation example Construction

Embodiment 13

Embodiment 30

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Abstract

Disclosed is a novel glycopeptide antibiotic derivative. The glycopeptide antibiotic derivative is characterized by having a sugar residue (I) represented by formula (I) [wherein n represents an integer of 1 to 5; Sug's independently represent a monosaccharide, and (Sug)n represents a bivalent sugar residue formed by binding 1 to 5 monosaccharides which are the same as or different from each other; RA1 represents a lower alkyl which may be substituted, a lower alkenyl which may be substituted, or a cycloalkyl which may be substituted; and RE represents OH or NHAc (wherein Ac represents an acetyl)] bound to an aromatic ring in the 4th amino acid residue located in a glycopeptide skeleton. The derivative has an antibacterial activity against a vancomycin-resistant bacterium.

Description

technical field The invention relates to glycosylated derivatives of glycopeptide antibiotics, a preparation method and intermediates thereof. Background technique Glycopeptide antibiotics are antibiotics with complex polycyclic peptide structures produced by various microorganisms and provide antibacterial drugs effective against most Gram-positive bacteria. In recent years, bacteria resistant to penicillins, cephalosporins, etc. have emerged, and infections caused by multidrug-resistant bacteria and methicillin-resistant Staphylococcus (MRSA) have caused serious problems in the medical field. Typically, glycopeptide antibiotics such as vancomycin are effective against such microorganisms, and vancomycin becomes a drug of last resort for infections caused by MRSA and other resistant bacteria. However, specific microorganisms such as vancomycin-resistant enterococci (VRE) are beginning to develop resistance to vancomycin. In addition, Staphylococcus aureus (VRSA) which has...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K9/00C07G11/00A61K38/00A61P9/00A61P31/04
CPCC07K9/008A61K38/00A61P11/00A61P17/00A61P19/02A61P31/04A61P9/00
Inventor 松井耕平皆川和之吉田修森元健次绪方雄贵
Owner SHIONOGI & CO LTD
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