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. 2018 May 30;9(6):552-556.
doi: 10.1021/acsmedchemlett.8b00103. eCollection 2018 Jun 14.

Riluzole-Triazole Hybrids as Novel Chemical Probes for Neuroprotection in Amyotrophic Lateral Sclerosis

Joseph B Sweeney  1 , Marcus Rattray  2 , Victoria Pugh  2   3 , Lucy A Powell  4
Affiliations

Riluzole-Triazole Hybrids as Novel Chemical Probes for Neuroprotection in Amyotrophic Lateral Sclerosis

Joseph B Sweeney et al. ACS Med Chem Lett. .

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.

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Conflict of interest statement

The authors declare no competing financial interest.

Figures

Figure 1
Figure 1
ALS drugs (1 and 2), neuroprotective small molecules (3, 4a, and 4b), and project target (5).
Scheme 1
Scheme 1. Click Chemical Strategy for Preparation of Triazole Library 5
See this image and copyright information in PMC

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