Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors

被引：83
|
作者：
Zhao, HY [1 ]
Liu, G
Xin, ZL
Serby, MD
Pei, ZH
Szczepankiewicz, BG
Hajduk, PJ
Abad-Zapatero, C
Hutchins, CW
Lubben, TH
Ballaron, SJ
Haasch, DL
Kaszubska, W
Rondinone, CM
Trevillyan, JM
Jirousek, MR
机构：
[1] Abbott Labs, Global Pharmaceut Res & Dev, Metab Dis Res, Abbott Pk, IL 60064 USA
[2] Abbott Labs, Global Pharmaceut Res & Dev, Adv Technol, Abbott Pk, IL 60064 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 22期
关键词：
PTP1B; selective; cell permeable;
D O I：
10.1016/j.bmcl.2004.08.063
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Guided by X-ray crystallography, we have extended the structure-activity relationship (SAR) study on an isoxazole carboxylic acid-based PTP1B inhibitor (1) and more potent and equally selective (>20-fold selectivity over the highly homologous T-cell PTPase, TCPTP) PTP1B inhibitors were identified. Inhibitor 7 demonstrated good cellular activity against PTP1B in COS 7 cells. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5543 / 5546
页数：4
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