2018年3月1日
Membrane-active antimicrobial poly(amino-modified alkyl) β-cyclodextrins synthesized via click reactions.
MedChemComm
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- 巻
- 9
- 号
- 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
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
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- DOI
- https://doi.org/10.1039/c7md00592j
- PubMed
- https://www.ncbi.nlm.nih.gov/pubmed/30108941
- PubMed Central
- https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6072522
- Scopus
- https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85044249794&origin=inward
- Scopus Citedby
- https://www.scopus.com/inward/citedby.uri?partnerID=HzOxMe3b&scp=85044249794&origin=inward
- ID情報
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- DOI : 10.1039/c7md00592j
- ISSN : 2040-2503
- eISSN : 2040-2511
- PubMed ID : 30108941
- PubMed Central 記事ID : PMC6072522
- SCOPUS ID : 85044249794