論文

査読有り
2018年

Membrane-active antimicrobial poly(amino-modified alkyl) β-cyclodextrins synthesized: Via click reactions

MedChemComm
  • Hatsuo Yamamura
  • ,
  • Miho Nonaka
  • ,
  • Shingo Okuno
  • ,
  • Ryogo Mitsuhashi
  • ,
  • Hisato Kato
  • ,
  • Takashi Katsu
  • ,
  • Kazufumi Masuda
  • ,
  • Koichi Tanimoto
  • ,
  • Haruyoshi Tomita
  • ,
  • Atsushi Miyagawa

9
3
開始ページ
509
終了ページ
518
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1039/c7md00592j
出版者・発行元
Royal Society of Chemistry

The emergence of drug-resistant bacteria has led to the high demand for new antibiotics. In this report, we investigated membrane-active antimicrobial β-cyclodextrins. These contain seven amino-modified alkyl groups on a molecule, which act as functional moieties to permeabilize bacterial cell membranes. The polyfunctionalization of cyclodextrins was achieved through a click reaction assisted by microwave irradiation. A survey using derivatives with systematically varied functionalities clarified the unique correlation of the antimicrobial activity of these compounds with their molecular structure and hydrophobicity/hydrophilicity balances. The optimum hydrophobicity for the compounds being membrane-active was specific to bacterial strains and animal cells
this led to specific compounds having selective toxicity against bacteria including multidrug-resistant pathogens. The results demonstrate that cyclodextrin is a versatile molecular scaffold for rationally designed structures and can be used for the development of new antibiotics.

リンク情報
DOI
https://doi.org/10.1039/c7md00592j

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