Riluzole–Triazole Hybrids as Novel Chemical Probes for Neuroprotection in Amyotrophic Lateral Sclerosis,ACS Medicinal Chemistry Letters

当前位置： X-MOL 学术 › ACS Med. Chem. Lett. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Riluzole–Triazole Hybrids as Novel Chemical Probes for Neuroprotection in Amyotrophic Lateral Sclerosis
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2018-05-30 00:00:00 , DOI: 10.1021/acsmedchemlett.8b00103
Joseph B. Sweeney ₁ , Marcus Rattray ₂ , Victoria Pugh _{2,

3} , Lucy A. Powell ₄

Affiliation

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.

中文翻译：

利鲁唑-三唑杂化物作为肌萎缩性侧索硬化症神经保护的新型化学探针

尽管生物医学和化学研究人员给予了极大的关注，但对肌萎缩性侧索硬化症（ALS）的批准治疗很少，目前仅向患者提供利鲁唑（Rilutek）和依达拉奉（Radicava）。此外，这些药物活性的机制基础目前尚不明确，限制了设计用于ALS的新药物的能力。这封信描述了含三唑的利鲁唑类似物的合成及其在新型神经保护性测定中的测试。鉴定出具有神经保护活性的七种化合物，其中两种化合物具有与利鲁唑相似的活性。

更新日期：2018-05-30

点击分享查看原文

点击收藏

公开下载

阅读更多本刊最新论文本刊介绍/投稿指南11