大环叔碳胺类β-分泌酶1（BACE-1）抑制剂的设计、合成及构效关系研究
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.
作者信息
Lindsley Stacey R, Moore Keith P, Rajapakse Hemaka A, Selnick Harold G, Young Mary Beth, Zhu Hong, Munshi Sanjeev, Kuo Lawrence, McGaughey Georgia B, Colussi Dennis, Crouthamel Ming-Chih, Lai Ming-Tain, Pietrak Beth, Price Eric A, Sankaranarayanan Sethu, Simon Adam J, Seabrook Guy R, Hazuda Daria J, Pudvah Nicole T, Hochman Jerome H, Graham Samuel L, Vacca Joseph P, Nantermet Philippe G
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA.
出版信息
Bioorg Med Chem Lett. 2007 Jul 15;17(14):4057-61. doi: 10.1016/j.bmcl.2007.04.072. Epub 2007 Apr 27.
This Letter describes the design and synthesis of tertiary carbinamine macrocyclic inhibitors of the beta-secretase (BACE-1) enzyme. These macrocyclic inhibitors, some of which incorporate novel P2 substituents, display a 2- to 100-fold increase in potency relative to the previously described acyclic analogs while affording greater stability.
本信函描述了β-分泌酶（BACE-1）酶的叔碳胺大环抑制剂的设计与合成。这些大环抑制剂中的一些含有新型P2取代基，与先前描述的非环状类似物相比，其效力提高了2至100倍，同时具有更高的稳定性。
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