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Synthesis of C-5a-chain extended derivatives of 4-epi-isofagomine: Powerful β-galactosidase inhibitors and low concentration activators of GM1-gangliosidosis-related human lysosomal β-galactosidase.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2016 Mar 01; Vol. 26 (5), pp. 1438-42. Date of Electronic Publication: 2016 Jan 22. - Publication Year :
- 2016
-
Abstract
- From an easily available partially protected formal derivative of 1-deoxymannojirimycin, by hydroxymethyl chain-branching and further elaboration, lipophilic analogs of the powerful β-d-galactosidase inhibitor 4-epi-isofagomine have become available. New compounds exhibit improved inhibitory activities comparable to benchmark compound NOEV (N-octyl-epi-valienamine) and may serve as leads towards improved and more selective pharmacological chaperones for GM1-gangliosidosis.<br /> (Copyright © 2016 Elsevier Ltd. All rights reserved.)
- Subjects :
- Dose-Response Relationship, Drug
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Gangliosidosis, GM1 pathology
Humans
Imino Pyranoses chemical synthesis
Imino Pyranoses chemistry
Lysosomes drug effects
Models, Molecular
Molecular Structure
Structure-Activity Relationship
beta-Galactosidase metabolism
Enzyme Inhibitors pharmacology
Gangliosidosis, GM1 enzymology
Imino Pyranoses pharmacology
Lysosomes enzymology
beta-Galactosidase antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 26
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 26838810
- Full Text :
- https://doi.org/10.1016/j.bmcl.2016.01.059