オキムラ　ケイコ   Keiko Okimura
  興村　桂子
   所属   薬学部 薬学科
   職種   准教授
言語種別 英語
発行・発表の年月 2007/12
形態種別 学術論文
査読 査読あり
標題 Semi-Synthesis of Polymyxin B (2-10) and Colistin (2-10) Analogs Employing the Trichloroethoxy-carbonyl (Troc) Group for Side Chain Protection of α,γ-Diaminobutyric Acid Residues
執筆形態 共著
掲載誌名 Chem. Pharm. Bull.
巻・号・頁 55,pp.1724-1730
著者・共著者 Keiko Okimura, Kazuhiro Ohki, Yuki Sato, Kuniharu Ohnishi, and Naoki Sakura
概要 Improved strategies for the chemical conversion of natural polymyxin B and colistin to their N-terminal analogs are reported. The new key compounds, tetrakis(Nγ-Troc)-polymyxin B (2-10) and tetrakis(Nγ-Troc)-colistin (2-10), were obtained in 19% and 15% yields, respectively, which is higher than previous reports using trifluoroacetyl (Tfa) for tetrakis(Nγ-Tfa)-polymyxin B (2-10) and tetrakis(Nγ-Tfa)-colistin (2-10), respectively. The various Nα-acylated polymyxin B (2-10) analogs showed slightly higher antimicrobial and LPS binding activities than the corresponding Nα-acylated colistin (2-10) analogs.