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Issue 2, 2016
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Synthesis and biological evaluation of D-gluconhydroximo-1,5-lactam and its oxime-substituted derivatives as pharmacological chaperones for the treatment of Gaucher disease

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Abstract

D-Gluconhydroximo-1,5-lactam and its oxime-substituted derivatives were prepared and assessed for inhibition and pharmacological chaperone (PC) activities in Gaucher disease cell lines derived from N370S. The most active compound, O-(D-glucopyranosylidene) amino-Z-N-dodecylcarbamate (38), gave a nearly 2.0-fold increase in N370S β-GCase activity at 12.5 μM with no inhibition to other commercially available glucosidases. Docking studies of ligand–enzyme interactions have also been conducted to account for the results of enzyme activity increase. All these results demonstrate that compound 38 is a promising PC for the treatment of GD.

Graphical abstract: Synthesis and biological evaluation of d-gluconhydroximo-1,5-lactam and its oxime-substituted derivatives as pharmacological chaperones for the treatment of Gaucher disease

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Publication details

The article was received on 02 Nov 2015, accepted on 12 Dec 2015 and first published on 15 Dec 2015


Article type: Research Article
DOI: 10.1039/C5MD00501A
Citation: Med. Chem. Commun., 2016,7, 365-370
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    Synthesis and biological evaluation of D-gluconhydroximo-1,5-lactam and its oxime-substituted derivatives as pharmacological chaperones for the treatment of Gaucher disease

    J. Wang, X. Wang, Y. Zhao, X. Ma, Y. Wan, Z. Chen, H. Chen, H. Gan, J. Li, L. Li, P. G. Wang and W. Zhao, Med. Chem. Commun., 2016, 7, 365
    DOI: 10.1039/C5MD00501A

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