Author/Authors :
Yuo-Ling Chou، نويسنده , , David D. Davey، نويسنده , , Keith A. Eagen، نويسنده , , Brian D. Griedel، نويسنده , , Rushad Karanjawala، نويسنده , , Gary B. Phillips، نويسنده , , Karna L. Sacchi، نويسنده , , Kenneth J. Shaw، نويسنده , , Shung C. Wu، نويسنده , , Dao Lentz، نويسنده , , Amy M. Liang، نويسنده , , Lan Trinh، نويسنده , , Michael M. Morrissey، نويسنده , , Monica J. Kochanny، نويسنده ,
Abstract :
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.
