Stable analogues of nojirimycin-synthesis and biological evaluation of nojiristegine and manno-nojiristegine

Agnete H. Viuff; Louise M. Besenbacher; Akiko Kamori; Mikkel T. Jensen; Mogens Kilian; Atsushi Kato; Henrik H. Jensen

doi:10.1039/c5ob01281c

Stable analogues of nojirimycin-synthesis and biological evaluation of nojiristegine and manno-nojiristegine

Agnete H. Viuff, Louise M. Besenbacher, Akiko Kamori, Mikkel T. Jensen, Mogens Kilian, Atsushi Kato, Henrik H. Jensen^*

^*この論文の責任著者

薬剤部

研究成果: ジャーナルへの寄稿 › 学術論文 › 査読

17 被引用数 (Scopus)

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Two novel iminosugars called nojiristegines, being structural hybrids between nor-tropane alkaloid calystegine and nojirimycins, have been synthesised and found to be stable molecules despite the presence of a hemiaminal functionality. The synthesised iminosugars were evaluated against a panel of glycosidases and the best inhibition (IC₅₀), found against α-glucosidases, was in the micromolar region. The compounds were also evaluated as potential antibiotics but no useful level of activity was observed.

本文言語	英語
ページ（範囲）	9637-9658
ページ数	22
ジャーナル	Organic and Biomolecular Chemistry
巻	13
号	37
DOI	https://doi.org/10.1039/c5ob01281c
出版ステータス	出版済み - 2015/07/14

ASJC Scopus 主題領域

生化学
物理化学および理論化学
有機化学

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10.1039/c5ob01281c

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title = "Stable analogues of nojirimycin-synthesis and biological evaluation of nojiristegine and manno-nojiristegine",

abstract = "Two novel iminosugars called nojiristegines, being structural hybrids between nor-tropane alkaloid calystegine and nojirimycins, have been synthesised and found to be stable molecules despite the presence of a hemiaminal functionality. The synthesised iminosugars were evaluated against a panel of glycosidases and the best inhibition (IC50), found against α-glucosidases, was in the micromolar region. The compounds were also evaluated as potential antibiotics but no useful level of activity was observed.",

author = "Viuff, {Agnete H.} and Besenbacher, {Louise M.} and Akiko Kamori and Jensen, {Mikkel T.} and Mogens Kilian and Atsushi Kato and Jensen, {Henrik H.}",

note = "Publisher Copyright: {\textcopyright} The Royal Society of Chemistry 2015.",

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day = "14",

doi = "10.1039/c5ob01281c",

language = "英語",

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T1 - Stable analogues of nojirimycin-synthesis and biological evaluation of nojiristegine and manno-nojiristegine

AU - Viuff, Agnete H.

AU - Besenbacher, Louise M.

AU - Kamori, Akiko

AU - Jensen, Mikkel T.

AU - Kilian, Mogens

AU - Kato, Atsushi

AU - Jensen, Henrik H.

PY - 2015/7/14

Y1 - 2015/7/14

N2 - Two novel iminosugars called nojiristegines, being structural hybrids between nor-tropane alkaloid calystegine and nojirimycins, have been synthesised and found to be stable molecules despite the presence of a hemiaminal functionality. The synthesised iminosugars were evaluated against a panel of glycosidases and the best inhibition (IC50), found against α-glucosidases, was in the micromolar region. The compounds were also evaluated as potential antibiotics but no useful level of activity was observed.

AB - Two novel iminosugars called nojiristegines, being structural hybrids between nor-tropane alkaloid calystegine and nojirimycins, have been synthesised and found to be stable molecules despite the presence of a hemiaminal functionality. The synthesised iminosugars were evaluated against a panel of glycosidases and the best inhibition (IC50), found against α-glucosidases, was in the micromolar region. The compounds were also evaluated as potential antibiotics but no useful level of activity was observed.

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U2 - 10.1039/c5ob01281c

DO - 10.1039/c5ob01281c

M3 - 学術論文

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AN - SCOPUS:84941906910

SN - 1477-0520

VL - 13

SP - 9637

EP - 9658

JO - Organic and Biomolecular Chemistry

JF - Organic and Biomolecular Chemistry

IS - 37

ER -

Stable analogues of nojirimycin-synthesis and biological evaluation of nojiristegine and manno-nojiristegine

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