1032767-29-5Relevant articles and documents
Sulfamide as Zinc Binding Motif in Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa)
Halland, Nis,Czech, J?rg,Czechtizky, Werngard,Evers, Andreas,Follmann, Markus,Kohlmann, Markus,Schreuder, Herman A.,Kallus, Christopher
, p. 9567 - 9573 (2016)
Previously disclosed TAFIa inhibitors having a urea zinc-binding motif were used as the starting point for the development of a novel class of highly potent inhibitors having a sulfamide zinc-binding motif. High-resolution X-ray cocrystal structures were used to optimize the structures and reveal a highly unusual sulfamide configuration. A selected sulfamide was profiled in vitro and in vivo and displayed a promising ADMET profile.