| Autor: |
Chao Wang, Guanyu Yang, Ping Xu, Yan Niu, Qi Sun, Peng Liu, Haifei Gao, Fengrong Xu |
| Rok vydání: |
2012 |
| Předmět: |
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| Zdroj: |
Chemical Biology & Drug Design. 80:775-780 |
| ISSN: |
1747-0277 |
| DOI: |
10.1111/cbdd.12016 |
| Popis: |
A series of 3, 5-disubstituted benzimidamides were synthesized and biologically evaluated as potential BACE1 inhibitors. Both the targeted compounds (benzimidamides) and the synthetic intermediates (benzonitriles) were tested for their BACE1 inhibitory activities in a cell-free FRET assay. All the synthesized benzimidamides were active as BACE1 inhibitors and compound 6d showed the lowest IC50 value of 3.35 μm. Molecular docking study proposed a binding mode, which would help to the further optimization on 6d to achieve more potent, BBB penetrant BACE1 inhibitors. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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