Title | Synthesis of C-5a-chain extended derivatives of 4-epi-isofagomine: Powerful beta-galactosidase inhibitors and low concentration activators of G(M1)-gangliosidosis-related human lysosomal beta-galactosidase |
Publication Type | Journal Article |
Year of Publication | 2016 |
Authors | Thonhofer, M, Weber, P, Santana, AGonzalez, Fischer, R, Pabst, BM, Paschke, E, Schalli, M, Stuetz, AE, Tschernutter, M, Windischhofer, W, Withers, SG |
Journal | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS |
Volume | 26 |
Pagination | 1438-1442 |
Date Published | MAR 1 |
ISSN | 0960-894X |
Abstract | From an easily available partially protected formal derivative of 1-deoxymannojirimycin, by hydroxymethyl chain-branching and further elaboration, lipophilic analogs of the powerful beta-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 G(M1)-gangliosidosis. (C) 2016 Elsevier Ltd. All rights reserved. |
DOI | 10.1016/j.bmcl.2016.01.059 |