Ontology highlight
ABSTRACT:
SUBMITTER: Shangguan S
PROVIDER: S-EPMC6269915 | biostudies-literature | 2013 Mar
REPOSITORIES: biostudies-literature
Shangguan Shihao S Wang Fei F Liao Yong Y Yu Haiping H Li Jia J Huang Wenhai W Hu Haihong H Yu Lushan L Hu Yongzhou Y Sheng Rong R
Molecules (Basel, Switzerland) 20130320 3
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 v ...[more]