Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
SHR Neuro Krebs Kardio Lipid Stoffw Microb
Weber, P; Fischer, R; Nasseri, SA; Pabst, BM; Prasch, H; Stuetz, AE; Thonhofer, M; Withers, SG; Windischhofer, W; Wrodnigg, TM.
N-Methyl-N-Alkylaminocyclopentanes: Powerful and Selective β-
HELV CHIM ACTA. 2024;
Doi: 10.1002/hlca.202300219
Web of Science
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- Co-Autor*innen der Med Uni Graz
- Pabst Bettina
- Windischhofer Werner
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- Abstract:
- Building upon a previously established (2+3)-cycloaddition strategy, a series of N,N-dialkylated aminocyclopentanes was synthesized using a partially protected eno-furanose as the starting point. The resulting N-methylisoxazolidine was subsequently transformed into the corresponding aminocyclopentane, which was further N-alkylated, yielding a collection of compounds with potential as inhibitors and pharmacological chaperones of beta-d-glucocerebrosidase. A comprehensive screening involving a range of biologically relevant glycosidases unveiled that these compounds exhibit remarkable potency and selectivity as inhibitors of human lysosomal beta-d-glucocerebrosidase. However, none of these compounds exhibit significant activity enhancement of Morbus Gaucher related p.N409S/p.L483P mutant beta-d-glucocerebrosidase.
- Find related publications in this database (Keywords)
- aminocyclopentanes
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beta-
d -glucocerebrosidase - carbohydrates
- glycosidase inhibitors
- pharmacological chaperones