Design and synthesis of potent, non-peptidic inhibitors of HPTPβ

被引:33
|
作者
Amarasinghe, Kande K. D.
Evidokimov, Artem G.
Xu, Kevin
Clark, Cynthia M.
Maier, Matthew B.
Srivastava, Anil
Colson, Anny-Odile
Gerwe, Gina S.
Stake, George E.
Howard, Brian W.
Pokross, Matthew E.
Gray, Jeffrey L.
Peters, Kevin G.
机构
[1] Procter & Gamble Pharmaceut, Hlth Care Res Ctr, Mason, OH 45040 USA
[2] Chembiotek Res Inst, Kolkata 700091, W Bengal, India
关键词
protein tyrosine phosphatases; HPTP beta; sulfamic acid; malonates; oxadiazoles; PROTEIN-TYROSINE PHOSPHATASES; ENDOTHELIAL GROWTH-FACTOR; ANGIOPOIETIN-1;
D O I
10.1016/j.bmcl.2006.05.074
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The sulfamic acid phosphotyrosine mimetic was coupled with a previously known malonate template to obtain highly selective and potent inhibitors of HPTP beta. Potentially hydrolyzable malonate ester functionalities were replaced with 1,2,4-oxadiazoles without a significant effect on HPTP beta potency. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4252 / 4256
页数:5
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