强效二苯并氮杂䓬基序作为β-分泌酶抑制剂的合理设计与合成
Rational design and synthesis of potent dibenzazepine motifs as beta-secretase inhibitors.
作者信息
Al-Tel Taleb H, Al-Qawasmeh Raed A, Schmidt Marco F, Al-Aboudi Amal, Rao Shashidhar N, Sabri Salim S, Voelter Wolfgang
机构信息
College of Pharmacy, University of Sharjah, P.O. Box 27272, Sharjah, UAE.
出版信息
J Med Chem. 2009 Oct 22;52(20):6484-8. doi: 10.1021/jm9008482.
We have identified small-molecule dibenzazepine inhibitors of beta-secretase (BACE1). These BACE1 inhibitors possess two key salient features. The first is a seven-membered heterocyclic ring fused to two aromatic rings representing the P3-P2 residues. The second is an amide and/or amide bioisostere representing the P1' residue. Rational optimization led to the identification of potent analogues, such as 10 (K(I) = 211 nM).
我们已经鉴定出β-分泌酶（BACE1）的小分子二苯并氮杂卓抑制剂。这些BACE1抑制剂具有两个关键的显著特征。第一个是与代表P3-P2残基的两个芳环稠合的七元杂环。第二个是代表P1'残基的酰胺和/或酰胺生物电子等排体。合理的优化导致鉴定出有效的类似物，例如10（K（I）= 211 nM）。
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