Issue 36, 2016

Synthesis and evaluation of N-alkylated analogues of aza-galacto-fagomine – potential pharmacological chaperones for Krabbe disease

Abstract

Seven novel alkylated or acylated analogues of hexahydropyridazine aza-galacto-fagomine (AGF) was prepared and studied as glycosidase inhibitors with the aim of increasing inhibitory potency and selectivity. The enzyme galactocerebrosidase, implicated in Krabbe disease, was found to be potently inhibited by n-butyl N2-alkylated AGF.

Graphical abstract: Synthesis and evaluation of N-alkylated analogues of aza-galacto-fagomine – potential pharmacological chaperones for Krabbe disease

Supplementary files

Article information

Article type
Paper
Submitted
17 Jun 2016
Accepted
08 Aug 2016
First published
08 Aug 2016

Org. Biomol. Chem., 2016,14, 8545-8556

Synthesis and evaluation of N-alkylated analogues of aza-galacto-fagomine – potential pharmacological chaperones for Krabbe disease

A. H. Viuff and H. H. Jensen, Org. Biomol. Chem., 2016, 14, 8545 DOI: 10.1039/C6OB01309K

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