发现新型 2,3-二氢-1H-茚-1-胺衍生物作为选择性单胺氧化酶 B 抑制剂。
Discovery of novel 2,3-dihydro-1H-inden-1-amine derivatives as selective monoamine oxidase B inhibitors.
机构信息
School of Food and Biological Engineering, Hefei University of Technology, Hefei, Anhui 230009, PR China.
School of Food and Biological Engineering, Hefei University of Technology, Hefei, Anhui 230009, PR China.
出版信息
Bioorg Med Chem Lett. 2019 May 1;29(9):1090-1093. doi: 10.1016/j.bmcl.2019.02.030. Epub 2019 Feb 27.
Inhibition of MAO-B has been an effective strategy for the treatment of Parkinson's disease. To find more potent and selective MAO-B inhibitors with novel chemical scaffold, we designed and synthesized a series of new 2,3-dihydro-1H-inden-1-amine derivatives on basis of our previous study. Furthermore, the corresponding structure-activity relationship (SAR) of these compounds is detailedly discussed. Compounds L4 (IC = 0.11 μM), L8 (IC = 0.18 μM), L16 (IC = 0.27 μM) and L17 (IC = 0.48 μM) showed similar MAO-B inhibitory activity as Selegiline. Moreover, L4, L16 and L17 also exhibited comparable selectivity with Selegiline, indicating that L4, L16 and L17 could be promising selective MAO-B inhibitors for further study.
抑制 MAO-B 一直是治疗帕金森病的有效策略。为了找到具有新型化学结构骨架的更有效和更具选择性的 MAO-B 抑制剂，我们在之前的研究基础上设计并合成了一系列新的 2,3-二氢-1H-茚-1-胺衍生物。此外，详细讨论了这些化合物的相应构效关系（SAR）。化合物 L4（IC=0.11μM）、L8（IC=0.18μM）、L16（IC=0.27μM）和 L17（IC=0.48μM）表现出与Selegiline 相似的 MAO-B 抑制活性。此外，L4、L16 和 L17 与 Selegiline 也具有相当的选择性，表明 L4、L16 和 L17 可能是有前途的选择性 MAO-B 抑制剂，值得进一步研究。
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