Sweeney Joseph B, Rattray Marcus, Pugh Victoria, Powell Lucy A
Department of Chemistry, Lancaster University, Lancaster LA1 4YB, U.K.
School of Pharmacy and Medical Sciences, University of Bradford, Bradford BD7 1DP, U.K.
ACS Med Chem Lett. 2018 May 30;9(6):552-556. doi: 10.1021/acsmedchemlett.8b00103. eCollection 2018 Jun 14.
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.
尽管生物医学和化学研究人员给予了高度关注，但目前针对肌萎缩侧索硬化症（ALS）的获批治疗方法很少，患者目前仅能使用利鲁唑（力如太）和依达拉奉（瑞必乐）。此外，这些药物活性的作用机制目前尚不清楚，这限制了设计治疗ALS新药的能力。本信函描述了含三唑的利鲁唑类似物的合成及其在一种新型神经保护试验中的测试。七种化合物被鉴定具有神经保护活性，其中两种化合物具有与利鲁唑相似的活性。
