Structural highlights
Publication Abstract from PubMed
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.
Sulfamide as Zinc Binding Motif in Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa).,Halland N, Czech J, Czechtizky W, Evers A, Follmann M, Kohlmann M, Schreuder HA, Kallus C J Med Chem. 2016 Oct 17. PMID:27749053[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Halland N, Czech J, Czechtizky W, Evers A, Follmann M, Kohlmann M, Schreuder HA, Kallus C. Sulfamide as Zinc Binding Motif in Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa). J Med Chem. 2016 Oct 17. PMID:27749053 doi:http://dx.doi.org/10.1021/acs.jmedchem.6b01276
