Synthesis and biological evaluations of novel bendazac lysine analogues as potent anticataract agents

被引：41

作者：

Shen, Hong ^{[1
]}

Gou, Shaohua ^{[1
,2
,3
]}

Shen, Jianping ^{[4
]}

Zhu, Yanqin ^{[4
]}

Zhang, Yindi ^{[4
]}

Chen, Xuetai ^{[1
]}

机构：

[1] Nanjing Univ, Sch Chem & Chem Engn, Nanjing 210093, Peoples R China

[2] Southeast Univ, Pharmaceut Res Ctr, Nanjing 211189, Peoples R China

[3] Southeast Univ, Sch Chem & Chem Engn, Nanjing 211189, Peoples R China

[4] Nanjing Med Univ, Inst Clin Pharmacol, Nanjing 210029, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 07期

关键词：

Bendazac lysine analogues; Anticataract agents; Aqueous solubility; SOLUBLE LENS PROTEINS; MOLECULAR CHAPERONE; POSSIBLE MECHANISM; ALPHA-CRYSTALLIN; CATARACT; SCAVENGER; STABILITY; DELAY; SALT;

D O I：

10.1016/j.bmcl.2010.02.061

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel bendazac analogues and their salts have been designed and prepared. The resulting compounds (13c-d, 15c, 17c) showed very good aqueous solubility (> 100 mg/mL). An in vitro assay showed that most of the resulting compounds had potent protective activity against the oxidative damage. Particularly, compound 13d was also able to enhance the WSP and T-AOC level in the H2O2/FeCl3-induced oxidative damage model, indicating the resulting compound may protect the lens through an antioxidant pathway. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：2115 / 2118

页数：4

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