期刊
MOLECULES
卷 18, 期 3, 页码 3577-3594出版社
MDPI
DOI: 10.3390/molecules18033577
关键词
BACE-1 inhibitor; 2-amino-6H-1,3,4-thiadizine; blood-brain barrier permeability
资金
- National Natural Science Foundation of China [21172193]
- Zhejiang Provincial Natural Foundation of China [R2110297]
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 beta-secretase (BACE-1) inhibitors. Preliminary structure-activity relationships revealed that the existence of a 2-amino-6H-1,3,4-thiadizine moiety and a-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 mu M 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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