780770-01-6Relevant academic research and scientific papers
Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif
Kreutter, Kevin D.,Lu, Tianbao,Lee, Lily,Giardino, Edward C.,Patel, Sharmila,Huang, Hui,Xu, Guozhang,Fitzgerald, Mark,Haertlein, Barbara J.,Mohan, Venkatraman,Crysler, Carl,Eisennagel, Stephen,Dasgupta, Malini,McMillan, Martin,Spurlino, John C.,Huebert, Norman D.,Maryanoff, Bruce E.,Tomczuk, Bruce E.,Damiano, Bruce P.,Player, Mark R.
, p. 2865 - 2870 (2008/12/21)
2-Cyano-6-fluorophenylacetamide was explored as a novel P2 scaffold in the design of thrombin inhibitors. Optimization around this structural motif culminated in 14, which is a potent thrombin inhibitor (Ki = 1.2 nM) that exhibits robust effica
