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

        1 , 2 , 2 , 3 , 4
      ACS Medicinal Chemistry Letters
      American Chemical Society (ACS)

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          Abstract

          <p class="first" id="d456794e188"> <div class="figure-container so-text-align-c"> <img alt="" class="figure" src="/document_file/41fb4c8d-0e0b-4a7f-bc9e-da1fc51138e7/PubMedCentral/image/ml-2018-00103y_0004"/> </div> </p><p id="d456794e192">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. </p>

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          Author and article information

          Journal
          ACS Medicinal Chemistry Letters
          ACS Med. Chem. Lett.
          American Chemical Society (ACS)
          1948-5875
          1948-5875
          May 16 2018
          June 14 2018
          May 30 2018
          June 14 2018
          : 9
          : 6
          : 552-556
          Affiliations
          [1 ]Department of Chemistry, Lancaster University, Lancaster LA1 4YB, U.K.
          [2 ]School of Pharmacy and Medical Sciences, University of Bradford, Bradford BD7 1DP, U.K.
          [3 ]School of Chemistry, Food &amp; Nutritional Sciences and Pharmacy, University of Reading, Reading, Berkshire RG6 6AP, U.K.
          [4 ]Department of Chemical Sciences, University of Huddersfield, Huddersfield HD1 3DH, U.K.
          Article
          10.1021/acsmedchemlett.8b00103
          6004570
          29937981
          ecf5a337-73c7-4bd3-b34b-ea20cb1dc348
          © 2018
          History

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