A series of β-secretase peptidomimetic inhibitors with Leu*Ala hydroxyethylene dipeptide isostere were synthesized and their β-secretase inhibitory activities were measured. The most potent compound N9 showed an in...A series of β-secretase peptidomimetic inhibitors with Leu*Ala hydroxyethylene dipeptide isostere were synthesized and their β-secretase inhibitory activities were measured. The most potent compound N9 showed an inhibitory rate of 59.66% (10 mg/mL). Compound N9 might be further modified by means of computational chemical methodology.展开更多
基金National Natural Science Foundation of China(Grant No.30772650 and 20772008).
文摘A series of β-secretase peptidomimetic inhibitors with Leu*Ala hydroxyethylene dipeptide isostere were synthesized and their β-secretase inhibitory activities were measured. The most potent compound N9 showed an inhibitory rate of 59.66% (10 mg/mL). Compound N9 might be further modified by means of computational chemical methodology.