1429022-33-2Relevant academic research and scientific papers
Design, synthesis and evaluation of 3-(2-Aminoheterocycle)-4- benzyloxyphenylbenzamide derivatives as BACE-1 inhibitors
Shangguan, Shihao,Wang, Fei,Liao, Yong,Yu, Haiping,Li, Jia,Huang, Wenhai,Hu, Haihong,Yu, Lushan,Hu, Yongzhou,Sheng, Rong
, p. 3577 - 3594 (2013/04/24)
Three series of 3-(2-aminoheterocycle)-4-benzyloxyphenylbenzamide derivatives, 2-aminooxazoles, 2-aminothiazoles, and 2-amino-6H-1,3,4-thiadizines were designed, synthesized and evaluated as β-secretase (BACE-1) inhibitors. Preliminary structure-activity relationships revealed that the existence of a 2-amino-6H-1,3,4-thiadizine moiety and α-naphthyl group were favorable for BACE-1 inhibition. Among the synthesized compounds, 5e exhibited the most potent BACE-1 inhibitory activity, with an IC50 value of 9.9 μM and it exhibited high brain uptake potential in Madin-Darby anine kidney cell lines (MDCK) and a Madin-Darby canine kidney-multidrug resistance 1 (MDCK-MDR1) model.
