Synthesis and structure-activity relationships of benzophenones as inhibitors of cathepsin D

被引：50
|
作者：
Whitesitt, CA
Simon, RL
Reel, JK
Sigmund, SK
Phillips, ML
Shadle, JK
Heinz, LJ
Koppel, GA
Hunden, DC
Lifer, SL
Berry, D
Ray, J
Little, SP
Liu, XD
Marshall, WS
Panetta, JA
机构：
[1] Lilly Research Laboratories, Eli Lilly and Company, Indianapolis
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 18期
关键词：
D O I：
10.1016/0960-894X(96)00393-9
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Non peptide inhibitors of cathepsin D, an aspartyl protease that has been implicated in many disease states including Alzheimer's disease, were prepared and evaluated. The most potent inhibitor of cathepsin D in this series was found to be (Z)-5-[[4-(4-benzoyl-3-hydroxy-2-propylphenoxy)methylphenyl]methylene]-2-thioxo-4-thiazolidinone (3f, IC50 = 210 nM). Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码：2157 / 2162
页数：6
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