Second Generation of Hydroxyethylamine BACE-1 Inhibitors: Optimizing Potency and Oral Bioavailability

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• 作者：Nicolas Charrier ; Brian Clarke ; Leanne Cutler ; Emmanuel Demont ; Colin Dingwall ; Rachel Dunsdon ; Philip East ; Julie Hawkins ; Colin Howes ; Ishrut Hussain ; Phil Jeffrey ; Graham Maile ; Rosalie Matico ; Jul
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：June 12, 2008
• 年：2008
• 卷：51
• 期：11
• 页码：3313 - 3317
• 全文大小：528K
• 年卷期：v.51,no.11(June 12, 2008)
• ISSN：1520-4804

文摘

BACE-1 inhibition has the potential to provide a disease-modifying therapy for the treatment of Alzheimer’s disease. Optimization of a first generation of BACE-1 inhibitors led to the discovery of novel hydroxyethylamines (HEAs) bearing a tricyclic nonprime side. These derivatives have nanomolar cell potency and are orally bioavailable.