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Chain-Branched Polyhydroxylated Octahydro-1H-Indoles as Potential Leads against Lysosomal Storage Diseases

Authors :
Juan C. Estévez
Marcos A. González
M. Carmen Villaverde
Yuki Hirokami
Atsushi Kato
Fredy Sussman
David Reza
Ramón J. Estévez
Source :
Pharmaceuticals, Vol 12, Iss 2, p 47 (2019)
Publication Year :
2019
Publisher :
MDPI AG, 2019.

Abstract

Here, the synthesis and glycosidase inhibition properties of the two first known 3-ethyloctahydro-1H-indole-4,5,6-triols are reported. This study shows the transformation of d-glucose into polyhydroxylated 1-(2-nitrocyclohexane) acetaldehydes, followed by a protocol involving the formation of the azacyclopentane ring. Results of inhibitory potency assays and docking calculations show that at least one of them could be a lead for optimization in the search for compounds that behave like folding chaperones in lysosomal storage diseases.

Details

Language :
English
ISSN :
14248247
Volume :
12
Issue :
2
Database :
Directory of Open Access Journals
Journal :
Pharmaceuticals
Publication Type :
Academic Journal
Accession number :
edsdoj.f52415d4bded4867b41f673a0748df2c
Document Type :
article
Full Text :
https://doi.org/10.3390/ph12020047