Diot Jennifer, García-Moreno M Isabel, Gouin Sébastien G, Ortiz Mellet Carmen, Haupt Karsten, Kovensky José
Laboratoire des Glucides UMR CNRS 6219, Institut de Chimie de Picardie, Faculté des Sciences, Université de Picardie Jules Verne, 33 rue Saint-Leu, 80039 Amiens Cedex 1, France.
Org Biomol Chem. 2009 Jan 21;7(2):357-63. doi: 10.1039/b815408b. Epub 2008 Nov 18.
A series of mono-, di- and tri-valent iminosugars based on oligoethylene scaffolds and N-substituted deoxynojirymicin epitopes have been synthesized by "click chemistry" to study the effect of multivalency on glycosidase inhibition. Biological evaluation evidenced differences in the inhibition trends as a function of the enzyme nature. The results demonstrate that multivalency can be used in some case to modulate both the affinity and the selectivity of glycosidase inhibition.
通过“点击化学”合成了一系列基于低聚亚乙基支架和N-取代脱氧野尻霉素表位的单、二和三价亚氨基糖，以研究多价性对糖苷酶抑制作用的影响。生物学评价证明，抑制趋势因酶的性质而异。结果表明，在某些情况下，多价性可用于调节糖苷酶抑制的亲和力和选择性。
