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Riluzole–Triazole Hybrids as Novel Chemical Probes for Neuroprotection in Amyotrophic Lateral Sclerosis
Sweeney, J.B. Rattray, Marcus Pugh, V. Powell, L.A.
Sweeney, J.B.
Rattray, Marcus
Pugh, V.
Powell, L.A.
Publication Date
2018-06-14
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© 2018 ACS. This document is the Accepted Manuscript version of a Published Work that appeared in final form in ACS Medicinal Chemistry Letters, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see https://doi.org/10.1021/acsmedchemlett.8b00103
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openAccess
Accepted for publication
2018-05-30
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Abstract
Despite intense attention from biomedical and chemical researchers, there are few approved treatments for amyotrophic lateral sclerosis (ALS), with only riluzole (Rilutek) and edaravone (Radicava) currently available to patients. Moreover, the mechanistic basis of the activity of these drugs is currently not well-defined, limiting the ability to design new medicines for ALS. This Letter describes the synthesis of triazole-containing riluzole analogues, and their testing in a novel neuroprotective assay. Seven compounds were identified as having neuroprotective activity, with two compounds having similar activity to riluzole.
Version
Accepted manuscript
Citation
Sweeney JB, Rattray M, Pugh V and Powell LA (2018) Riluzole-Triazole Hybrids as Novel Chemical Probes for Neuroprotection in Amyotrophic Lateral Sclerosis. ACS Medicinal Chemistry Letters. 9(6): 552-556.
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Letter