Format:
Online-Ressource
ISSN:
1522-2675
Content:
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 β‐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 β‐d‐glucocerebrosidase. However, none of these compounds exhibit significant activity enhancement of Morbus Gaucher related p.N409S/p.L483P mutant β‐d‐glucocerebrosidase.
In:
day:29
In:
month:02
In:
year:2024
In:
extent:10
In:
Helvetica chimica acta, New York, NY : Wiley-VCH, 1918-, (29.02.2024) (gesamt 10), 1522-2675
Language:
English
DOI:
10.1002/hlca.202300219
URN:
urn:nbn:de:101:1-2024022914562219834260
URL:
https://doi.org/10.1002/hlca.202300219
URL:
https://nbn-resolving.org/urn:nbn:de:101:1-2024022914562219834260
URL:
https://d-nb.info/1322098042/34
URL:
https://doi.org/10.1002/hlca.202300219
