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Synthesis and Biological Evaluation of Glycosidase Inhibitors: gem-Difluoromethylenated Nojirimycin Analogues

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Forfattere:
  • Bols, Mikael ;
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    Department of Chemistry, Faculty of Science, Aarhus University, Aarhus University
  • Wang, Ruo-Wen ;
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    Shanghai Institute of Organic Chemistry
  • Qiu, Xiao-Long ;
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    Shanghai Institute Organic of Chemistry
  • Ortega-Caballero, Fernando ;
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    Aarhus Universitet
  • Qing, Feng-Ling
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    Shanghia Institute of Organic Chemistry
Resumé:
In our ongoing program aimed at the design, synthesis, and biological evaluation of novel gem-difluoromethylenated glycosidase inhibitors, gem-4,4-difluoromethylenated iminosugars (5-9) were synthesized. The biological evaluation of these synthetic iminosugars showed that the gem-difluoromethylenyl group generally reduced the inhibition of glycosidases. However, this was not the case at pH 5.0, where the gem-difluoromethylenated iminosugar 6 was a stronger inhibitor than comparable iminosugars 1 and 36, suggesting that the influence of this group is mainly through its effect on the amine. It is proposed that the unprotonated iminosugar is the species preferably bound by beta-glucosidase, due to the lower pK(a) value of iminosugar 6 than of 1 or 36, leaving iminosugars 1 and 36 mostly protonated at pH 5.0, while iminosugar 6 is not. Iminosugar 6 also displayed good and selective inhibition of beta-glucosidase at pH 6.8.
Type:
Tidsskrift-artikel
Sprog:
Engelsk
Udgivet i:
J. Med. Chem, 2006, Vol 49, p. 2989-2997
Hovedforskningsområde:
Science/technology
Publikationsstatus:
Publiceret
Review type:
Peer Review
Indberetningsår:
2006
Videnskabeligt niveau:
Videnskabelig
ID:
49039962
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