1449221-74-2Relevant articles and documents
4-Oxo-1,4-dihydro-quinoline-3-carboxamides as BACE-1 inhibitors: Synthesis, biological evaluation and docking studies
Liu, Peng,Niu, Yan,Wang, Chao,Sun, Qi,Zhai, Yaya,Yu, Jiapei,Sun, Jing,Xu, Fengrong,Yan, Gang,Huang, Wenjie,Liang, Lei,Xu, Ping
, p. 413 - 421 (2014/05/06)
In this work, we report a series of new 4-oxo-1,4-dihydro-quinoline-3- carboxamide derivatives as β-secretase (BACE-1) inhibitors. Supported by docking study, a small library of derivatives were designed, synthesized and biologically evaluated in vitro. The studies revealed that the most potent analog 14e (IC50 = 1.89 μM) with low cellular cytotoxicity and high predicted blood brain barrier permeability, could serve as a good structure for further modification.