期刊
CHEMICAL BIOLOGY & DRUG DESIGN
卷 93, 期 5, 页码 926-933出版社
WILEY
DOI: 10.1111/cbdd.13489
关键词
Alzheimer's disease; aminopyrimidine; BACE1 inhibitors; diaminopyrimidine
资金
- Specialized Research Fund for the Doctoral Program of Higher Education of China [20120001110010]
- National Natural Science Foundation of China [21002002, 21172012]
A series of novel aminopyrimidine and diaminopyrimidine derivatives were designed and optimized to improve their potency and permeability relative to lead compound 1 (IC50 = 37.4 mu M), which was discovered in a previous virtual screening. The potency of the optimized compound, 13g (IC50 = 1.4 mu M), was 26-fold greater than that of 1 based on a fluorescence resonance energy transfer assay, and a parallel artificial membrane permeability assay suggested that it could pass through the blood-brain barrier. Additionally, several compounds containing selenium showed good potencies and deserve further investigation as anti-Alzheimer's agents.
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