Riluzole-triazole hybrids as novel chemical probes for neuroprotection in amyotrophic lateral sclerosis

Sweeney, J. B., Rattray, M., Pugh, V. and Powell, L. A. (2018) Riluzole-triazole hybrids as novel chemical probes for neuroprotection in amyotrophic lateral sclerosis. ACS Medicinal Chemistry Letters, 9 (6). pp. 552-556. ISSN 1948-5875 doi: 10.1021/acsmedchemlett.8b00103

Abstract/Summary

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.