Molecules p. 3577 - 3594 (2013)
Update date:2022-08-04
Topics:
Shangguan, Shihao
Wang, Fei
Liao, Yong
Yu, Haiping
Li, Jia
Huang, Wenhai
Hu, Haihong
Yu, Lushan
Hu, Yongzhou
Sheng, Rong
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.
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Doi:10.1002/anie.201209959
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