强效且具选择性的BACE1间苯二甲酰胺S2羟乙胺抑制剂。
Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1.
作者信息
Kortum Steven W, Benson Timothy E, Bienkowski Michael J, Emmons Thomas L, Prince D Bryan, Paddock Donna J, Tomasselli Alfredo G, Moon Joseph B, LaBorde Alice, TenBrink Ruth E
机构信息
Pfizer Global Research and Development, Pfizer Inc., St. Louis Laboratories, 700 Chesterfield Parkway West, Chesterfield, MO 63017, USA.
出版信息
Bioorg Med Chem Lett. 2007 Jun 15;17(12):3378-83. doi: 10.1016/j.bmcl.2007.03.096. Epub 2007 Apr 3.
PMID:17434734
Abstract
The design and synthesis of a novel series of potent BACE1 hydroxyethylamine inhibitors. These inhibitors feature hydrogen bonding substituents at the C-5 position of the isophthalamide ring with improved selectivity over cathepsin D.
摘要
新型强效β-分泌酶1（BACE1）羟乙胺抑制剂的设计与合成。这些抑制剂在间苯二甲酰胺环的C-5位具有氢键取代基，对组织蛋白酶D具有更高的选择性。
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