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ID: ALA3860098
Journal: J Med Chem
Title: Sulfamide as Zinc Binding Motif in Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa).
Authors: Halland N, Czech J, Czechtizky W, Evers A, Follmann M, Kohlmann M, Schreuder HA, Kallus C.
Abstract: 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.
CiteXplore: 27749053