Chain-branched polyhydroxylated Octahydro-1H-Indoles as potential leads against lysosomal storage diseases
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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
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Estévez, J.C.; González, M.A.; Villaverde, M.C.; Hirokami, Y.; Kato, A.; Sussman, F.; Reza, D.; Estévez, R.J. Chain-Branched Polyhydroxylated Octahydro-1H-Indoles as Potential Leads against Lysosomal Storage Diseases. Pharmaceuticals 2019, 12, 47
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https://doi.org/10.3390/ph12020047Sponsors
This work has received financial support from the Spanish Ministry of Science and Innovation
(CTQ2009-08490), the Xunta de Galicia (Centro Singular de Investigación de Galicia, accreditation 2016–2019,
ED431B 2018/13; Project CN2011/037 and Project GRC2014/040), and the European Union (European Regional
Development Fund-ERDF). It has also received a Grant-in-Aid for Scientific Research (C) from the Japanese Society
for the Promotion of Science (JSPS KAKENHI Grant Number JP17K08362) (AK)
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© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)