Bioorganic Chemistry, 140, 106819: 1-14 (2023)

IF 5,1

Highly functionalized diaminocyclopentanes: A new route to potent and selective inhibitors of human O-GlcNAcase

Patrick Weber, Zuzana Mészáros, Pavla Bojarová, Manuel Ebner, Roland Fischer, Vladimír  Křen, Natalia Kulik, Philipp Müller, Miluše Vlachová, Kristýna Slámová, Arnold E. Stütz, Martin Thonhofer, Ana Torvisco, Tanja M. Wrodnigg, Andreas Wolfsgruber

 Abstract

A new class of compounds inhibiting de-O-glycosylation of proteins has been identified. Highly substituted diaminocyclopentanes are impressively selective reversible non-transition state O-β-N-acetyl-D-glucosaminidase (O-GlcNAcase) inhibitors. The ease of preparative access and remarkable biological activities provide highly viable leads for the development of anti-tau-phosphorylation agents with a view to eventually ameliorating Alzheimer’s disease.

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