183307-56-4Relevant academic research and scientific papers
Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors
Phillips, Gary,Davey, David D.,Eagen, Keith A.,Koovakkat, Sunil K.,Liang, Amy,Ng, Howard P.,Pinkerton, Michael,Trinh, Lan,Whitlow, Marc,Beatty, Alicia M.,Morrissey, Michael M.
, p. 1749 - 1756 (1999)
A novel series of 2,6-diphenoxypyridines has been designed to inhibit factor Xa, a serine protease strategically located in the coagulation cascade. The evolution from the photochemically unstable bisamidine (Z,Z)- BABCH to potent bisamidine compounds with a pyridine heterocycle as the core scaffold has been achieved. The most potent compound in the series, 6h, has a K(i) for human factor Xa of 12 nM. The selectivity of 6h against bovine trypsin and human thrombin was greater than 90- and 1000-fold, respectively. Two proposed modes of binding of 6h to factor Xa are made based on the crystal structures of 6h by itself and of 6h bound to bovine trypsin.
Benzamidine derivatives and their use as anti-coagulants
-
Page column 39, (2010/02/04)
This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
