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Biphenyls as potent vitronectin receptor antagonists.
Authors:Klaus Urbahns  Michael H?rter  Markus Albers  Delf Schmidt  Beatrix Stelte-Ludwig  Ulf Brüggemeier  Andrea Vaupel  Christoph Gerdes
Affiliation:Institute of Medicinal Chemistry, Pharma Research Centre, Bayer AG, D-42096 Wuppertal, FRG. klaus.urbahns.ku1@bayer.co.jp
Abstract:Vitronectin receptor (alpha(V)beta(3)) antagonism has been implicated as a mechanism for the treatment of restenosis following balloon angioplasty. In this work we present results from screening of a focused combinatorial library based on a biphenyl moiety. Our SAR studies led to the identification of compounds with subnanomolar activity, selectivity towards the related GPIIbIIIa receptor and functional activity on human smooth muscle cell migration.
Keywords:
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