Biphenyls as potent vitronectin receptor antagonists.: Part 3:: Squaric acid amides

被引：15
|
作者：
Urbahns, Klaus
Haerter, Michael
Albers, Markus
Schmidt, Delf
Stelte-Ludwig, Beatrix
Brueggemeier, Ulf
Vaupel, Andrea
Keldenich, Joerg
Lustig, Klemens
Tsujishita, Hideki
Gerdes, Christoph
机构：
[1] Bayer Schering Pharma, Bayer Hlthcare AG, Inst Med Chem, D-42096 Wuppertal, Germany
[2] Bayer AG, Combinat Chem Grp, D-51368 Leverkusen, Germany
[3] Bayer Schering Pharma, Bayer Hlthcare AG, Inst Lead Discovery, D-42096 Wuppertal, Germany
[4] Bayer Schering Pharma, Bayer Hlthcare AG, Inst Prot Therapeut, D-42096 Wuppertal, Germany
[5] Bayer Schering Pharma, Bayer Hlthcare AG, Inst Drug Metab & Pharmacol, D-42096 Wuppertal, Germany
[6] Bayer Yakutin Res Ctr, Dept Med Chem, Kyoto, Japan
[7] Bayer Schering Pharma, Bayer Hlthcare AG, Inst Cardiol Hematol, D-42096 Wuppertal, Germany
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 22期
关键词：
vitronectin; urea; arginine; guanidine mimetic; squaric acid amide; alpha nu beta(3); RGD; restenosis; biphenyl; smooth muscle cell;
D O I：
10.1016/j.bmcl.2007.09.039
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Vitronectin receptor (alpha(V)beta 3) antagonists have been implicated as a possible new treatment of restenosis following balloon angioplasty. In this work we investigate a series of novel arginine mimetic scaffolds leading to new insight of the alpha(V)beta 3/ligand interaction. Squaric acid amide 10 is a subnanomolar alpha(V)beta 3 antagonist with improved potency on human smooth muscle cell migration. (C) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：6151 / 6154
页数：4
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