Design and synthesis of conformationally restricted inhibitors of active thrombin activatable fibrinolysis inhibitor (TAFIa)

…, A Dahlén, T Olsson, M Polla, T Svensson

Index: Brink, Mikael; Dahlen, Anders; Olsson, Thomas; Polla, Magnus; Svensson, Tor Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 7 p. 2261 - 2268

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Citation Number: 4

Abstract

Abstract A series of 4, 5, 6, 7-tetrahydro-1H-benzimidazole-5-carboxylic acid and 5, 6, 7, 8- tetrahydroimidazo [1, 2-a] pyridine-7-carboxylic acid derivatives designed as inhibitors of TAFIa has been prepared via a common hydrogenation–alkylation sequence starting from the appropriate benzimidazole and imidazopyridine system. We present a successful design strategy using a conformational restriction approach resulting in potent and selective ...