1032764-91-2Relevant academic research and scientific papers
Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin
Halland, Nis,Br?nstrup, Mark,Czech, J?rg,Czechtizky, Werngard,Evers, Andreas,Follmann, Markus,Kohlmann, Markus,Schiell, Matthias,Kurz, Michael,Schreuder, Herman A.,Kallus, Christopher
, p. 4839 - 4844 (2015/06/23)
Anabaenopeptins isolated from cyanobacteria were identified as inhibitors of carboxypeptidase TAFIa. Cocrystal structures of these macrocyclic natural product inhibitors in a modified porcine carboxypeptidase B revealed their binding mode and provided the basis for the rational design of small molecule inhibitors with a previously unknown central urea motif. Optimization based on these design concepts allowed for a rapid evaluation of the SAR and delivered potent small molecule inhibitors of TAFIa with a promising overall profile.
UREA AND SULFAMIDE DERIVATIVES AS INHIBITORS OF TAFIa
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Page/Page column 29, (2010/03/02)
The invention relates to compounds of the formula I as defined herein, which are inhibitors of activated thrombin-activatable fibrinolysis inhibitor. The compounds of the formula I are suitable for manufacturing medicaments for the prophylaxis, secondary prevention and therapy of one or more disorders which are associated with thromboses, embolisms, hypercoagulability or fibrotic changes.
