Structure–Activity Studies of N‐Butyl‐1‐deoxynojirimycin (NB‐DNJ) Analogues: Discovery of Potent and Selective Aminocyclopentitol Inhibitors of GBA1 and GBA2

Analogues of N‐butyl‐1‐deoxynojirimycin (NB‐DNJ) were prepared and assayed for inhibition of ceramide‐specific glucosyltransferase (CGT), non‐lysosomal β‐glucosidase 2 (GBA2) and the lysosomal β‐glucosidase 1 (GBA1). Compounds 5 a–6 f, which carry sterically demanding nitrogen substituents, and comp...

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Veröffentlicht in:	ChemMedChem 2017-12, Vol.12 (23), p.1977-1984
Hauptverfasser:	Gu, Xingxian, Gupta, Vijayalaxmi, Yang, Yan, Zhu, Jin‐Yi, Carlson, Erick J., Kingsley, Carolyn, Tash, Joseph S., Schönbrunn, Ernst, Hawkinson, Jon, Georg, Gunda I.
Format:	Artikel
Sprache:	eng
Schlagworte:	1-Deoxynojirimycin - analogs & derivatives 1-Deoxynojirimycin - chemistry 1-Deoxynojirimycin - pharmacology Amino Alcohols - chemistry Amino Alcohols - pharmacology aminocyclitols Analogs beta-Glucosidase - antagonists & inhibitors beta-Glucosidase - metabolism Ceramide Cyclopentane Cyclopentanes - chemistry Cyclopentanes - pharmacology Dose-Response Relationship, Drug Drug Discovery enzyme inhibition Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Glucosyltransferase Humans Inhibition Inhibitors lysosomal glucosidase 1 Molecular Conformation N-butyl-1-deoxynojirimycin Nitrogen non-lysosomal glucosidase 2 Stereochemistry Structure-Activity Relationship Substitutes
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