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Second-generation iminoxylitol-based pharmacological chaperones for the treatment of Gaucher disease.

著者 Oulaïdi F , Front-Deschamps S , Gallienne E , Lesellier E , Ikeda K , Asano N , Compain P , Martin OR
ChemMedChem.2011 Feb 7 ; 6(2):353-61.
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ICOA, UMR 6005, Université d'Orléans et CNRS rue de Chartres, BP 6759, 45067 Orléans, France.

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A series of O-alkyl iminoxylitol derivatives was synthesized and evaluated as β-glucocerebrosidase (GCase) inhibitors. This structure-activity study shows a dramatic influence of the position of the alkyl chain (α-C1, O2, O3, or O4) on human GCase inhibition. Remarkably, 1,2-shift of the alkyl chain from C1 to O2 was found to maintain high inhibitory potency toward GCase as well as chaperone activity at sub-inhibitory concentration (10 nM). Removal of the stereogenic center at the pseudo-anomeric position led to shorter and more practical synthetic sequences. 2-O-Alkyl iminoxylitol derivatives constitute a new promising class of leads for the treatment of Gaucher disease by means of pharmacological chaperone therapy.
PMID: 21275057 [PubMed - indexed for MEDLINE]
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