229342-57-8Relevant academic research and scientific papers
Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors
Ye, Bin,Arnaiz, Damian O.,Chou, Yuo-Ling,Griedel, Brian D.,Karanjawala, Rushad,Lee, Wheeseong,Morrissey, Michael M.,Sacchi, Kama L.,Sakata, Steven T.,Shaw, Kenneth J.,Wu, Shung C.,Zhao, Zuchun,Adler, Marc,Cheeseman, Sarah,Dole, William P.,Ewing, Janice,Fitch, Richard,Lentz, Dao,Liang, Amy,Light, David,Morser, John,Post, Joseph,Rumennik, Galina,Subramanyam, Babu,Sullivan, Mark E.,Vergona, Ron,Walters, Janette,Wang, Yi-Xin,White, Kathy A.,Whitlow, Marc,Kochanny, Monica J.
, p. 2967 - 2980 (2008/02/07)
There remains a high unmet medical need for a safe oral therapy for thrombotic disorders. The serine protease factor Xa (fXa), with its central role in the coagulation cascade, is among the more promising targets for anticoagulant therapy and has been the
Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors
Chou, Yuo-Ling,Davey, David D.,Eagen, Keith A.,Griedel, Brian D.,Karanjawala, Rushad,Phillips, Gary B.,Sacchi, Karna L.,Shaw, Kenneth J.,Wu, Shung C.,Lentz, Dao,Liang, Amy M.,Trinh, Lan,Morrissey, Michael M.,Kochanny, Monica J.
, p. 507 - 511 (2007/10/03)
Compound 1 was identified by high throughput screening as a novel, potent, non-amidine factor Xa inhibitor with good selectivity against thrombin and trypsin. A series of modifications of the three aromatic groups of 1 was investigated. Substitution of chlorine or bromine for fluorine on the aniline ring led to the discovery of subnanomolar factor Xa inhibitors. Positions on the anthranilic acid ring that can accommodate further substitution were also identified.
