Syntheses and Selective Inhibitory Activities of Terphenyl??Bisamidines for Serine Proteases

W von der Saal, RA Engh, A Eichinger…

Index: Von Der Saal, Wolfgang; Engh, Richard A.; Eichinger, Andreas; Gabriel, Bernhard; Kucznierz, Ralf; Sauer, Juergen Archiv der Pharmazie, 1996 , vol. 329, # 2 p. 73 - 82

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Citation Number: 19

Abstract

Abstract Biphenyl nitriles 5a—c, terphenyl dinitriles 11a—d, and naphthalene-bis (benzonitrile) 11e were prepared by palladium-catalyzed cross coupling reactions and subsequently converted to biphenyl amidines 8a—c and bis (benzamidines) 4a—e. Among the biphenyl amidines 8 only the meta-derivative 8b inhibits factor Xa and trypsin (K i= 10 μM). The terphenyl bisamidine 4c does not inhibit factor Xa, trypsin, thrombin, and plasmin ...