183307-65-5Relevant academic research and scientific papers
Benzamidine derivatives and their use as anti-coagulants
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Page column 40, (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.
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 (2007/10/03)
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.
