4-Oxo-1, 4-dihydro-quinoline-3-carboxamides as BACE-1 inhibitors: Synthesis, biological evaluation and docking studies

P Liu, Y Niu, C Wang, Q Sun, Y Zhai, J Yu, J Sun…

Index: Liu, Peng; Niu, Yan; Wang, Chao; Sun, Qi; Zhai, Yaya; Yu, Jiapei; Sun, Jing; Xu, Fengrong; Yan, Gang; Huang, Wenjie; Liang, Lei; Xu, Ping European Journal of Medicinal Chemistry, 2014 , vol. 79, p. 413 - 421

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Citation Number: 8

Abstract

Abstract 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 (IC 50= 1.89 μM) with low cellular cytotoxicity and high predicted blood brain barrier permeability, could serve as a good structure for further ...