Bioorganic & Medicinal Chemistry Letters 2007-11-15

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

Klaus Urbahns, Michael Härter, Markus Albers, Delf Schmidt, Beatrix Stelte-Ludwig, Ulf Brüggemeier, Andrea Vaupel, Jörg Keldenich, Klemens Lustig, Hideki Tsujishita, Christoph Gerdes

Index: Bioorg. Med. Chem. Lett. 17(22) , 6151-4, (2007)

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Abstract

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.