Synthesis and biological evaluation of novel N-(alkoxyphenyl)-aminocarbonylbenzoic acid derivatives as PTP1B inhibitors

被引：7
|
作者：
Tong, Yuan Feng [1 ,2 ]
Zhang, Pei [1 ,2 ]
Chen, Feng [1 ,2 ]
Hao, Ling Hua [1 ,2 ]
Ye, Fei [2 ,3 ]
Tian, Jin Ying [2 ,3 ]
Wu, Song [1 ,2 ]
机构：
[1] Peking Union Med Coll, Inst Mat Med, Minist Hlth PRC, Key Lab Biosynth Nat Prod,Dept New Drug Res & Dev, Beijing 100050, Peoples R China
[2] Chinese Acad Med Sci, Beijing 100050, Peoples R China
[3] Peking Union Med Coll, Inst Mat Med, Dept Pharmacol, Beijing 100050, Peoples R China
来源：
CHINESE CHEMICAL LETTERS | 2010年 / 21卷 / 12期
基金：
高等学校博士学科点专项科研基金;
关键词：
Petroselinic acid; PTP1B; N-(Alkoxyphenyl)-aminocarbonylbenzoic acid derivatives; Synthesis; Diabetes; TYROSINE-PHOSPHATASE; 1B; INSULIN SENSITIVITY; RESISTANCE; DISCOVERY;
D O I：
10.1016/j.cclet.2010.07.005
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Based on the fact that petroselinic acid showed good inhibitory activity (IC50 = 6.99 mu mol/L) against protein tyrosine phophatase 1B(PTP1B) in vitro, a series of novel N-(alkoxyphenyl)-aminocarbonylbenzoic acid derivatives were designed and synthesized. The results indicated that most of the derivatives showed more potent activities against PTP1B. Especially, compound 13 had obvious activity with an IC50 of 106 nmol/L in vitro. (C) 2010 Song Wu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
引用
收藏
页码：1415 / 1418
页数：4
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