N63-carboxamides of N15-alkyl and N15, N15-dialkyl derivatives of teicoplanin and deglucoteicoplanin.

• MALABARBA ADRIANO

  Marion Merrell Dow Research Institute, Lepetit Research Center

• CIABATTI ROMEO

  Marion Merrell Dow Research Institute, Lepetit Research Center

• KETTENRING JÜRGEN

  Marion Merrell Dow Research Institute, Lepetit Research Center

• SCOTTI ROBERTO

  Marion Merrell Dow Research Institute, Lepetit Research Center

• CANDIANI GIAMPAOLO

  Marion Merrell Dow Research Institute, Lepetit Research Center

• BERTI MARISA

  Marion Merrell Dow Research Institute, Lepetit Research Center

• PALLANZA ROSA

  Marion Merrell Dow Research Institute, Lepetit Research Center

• GOLDSTEIN BETH P.

  Marion Merrell Dow Research Institute, Lepetit Research Center

抄録

The synthesis and biological properties of a series of N⁶³-carboxamides of 15-N-alkylated derivatives of teicoplanin A2 (CTA) and its aglycone (TD) are described. Among the compounds, those carrying hydrophilic groups or ionizable amino functions on the N¹⁵-alkyl chain are more soluble in water than parent N¹⁵-methylated or unmodified amides.<br> Selected compounds were more active in vitro than CTA or TD, and a few of them were also slightly more efficacious in vivo than the parent antibiotics in streptococcal septicemia in the mouse. Their degree of activity varied with the structure and length of the N¹⁵-alkyl chains.

収録刊行物

• The Journal of Antibiotics

  The Journal of Antibiotics 46 (4), 668-675, 1993

  公益財団法人 日本感染症医薬品協会

キーワード

• Drug Discovery
• Pharmacology

詳細情報

• CRID: 1390282679126972544
• NII論文ID: 130003502523
• DOI: 10.7164/antibiotics.46.668
• ISSN: 18811469
• ISSN: 00218820
• PubMed: 8501009
• 本文言語コード: en
• データソース種別:
  • JaLC
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可