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Synthesis and activity of hydroxyethylene peptidomimetic inhibitors of human β-secretase

Chao Ma, Yue-Hua Wang, Xiao-Ming Yang, Xiao-Min Zou,Yang Lü, Guan-Hua Du, Ping Xu*   

  1. 1. Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China;
    2. Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, China
  • Received:2008-04-19 Revised:2008-08-10 Online:2008-09-15 Published:2008-09-15
  • Contact: Ping Xu*

Abstract: 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.

Key words: β-Secretase inhibitors, β-Secretase inhibitors, Hydroxyethylene isostere, Hydroxyethylene isostere, Synthesis, Synthesis, Bioactivity, Bioactivity

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