通过利用采用统一合成方法制备的多种结构单元来拓展β-分泌酶1（BACE1）抑制剂的构效关系。
Expansion of the structure-activity relationships of BACE1 inhibitors by harnessing diverse building blocks prepared using a unified synthetic approach.
作者信息
Mayol-Llinàs Joan, Chow Shiao, Nelson Adam
机构信息
School of Chemistry , University of Leeds , Leeds , LS2 9JT , UK . Email:
Astbury Centre for Structural Molecular Biology , University of Leeds , Leeds , LS2 9JT , UK.
出版信息
Medchemcomm. 2019 Mar 22;10(4):616-620. doi: 10.1039/c9md00085b. eCollection 2019 Apr 1.
Abstract
The structural diversity of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors was expanded by harnessing diverse building blocks that had been prepared a unified lead-oriented synthetic approach. It was shown that the lipophilic cyclohexylmethyl group within a known series of BACE1 inhibitors could be productively replaced with a range of alternative ring systems.
摘要
通过利用采用统一的导向性先导化合物合成方法制备的多种结构单元，β位点淀粉样前体蛋白裂解酶1（BACE1）抑制剂的结构多样性得到了扩展。结果表明，在一系列已知的BACE1抑制剂中，亲脂性的环己基甲基可以有效地被一系列其他环状体系取代。
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