Author/Authors :
Joanne M. Smallheer، نويسنده , , Richard S. Alexander، نويسنده , , Jianmin Wang، نويسنده , , Shuaige Wang، نويسنده , , Suanne Nakajima، نويسنده , , Karen A. Rossi، نويسنده , , Angela Smallwood، نويسنده , , Frank Barbera، نويسنده , , Debra Burdick، نويسنده , , Joseph M. Luettgen، نويسنده , , Robert M. Knabb، نويسنده , , Ruth R. Wexler، نويسنده , , Prabhakar K. Jadhav، نويسنده ,
Abstract :
Modifications to the P4 moiety and pyrazole C3 substituent of factor Xa inhibitor SN-429 provided several new compounds, which are 5–10 nM inhibitors of factor IXa. An X-ray crystal structure of one example complexed to factor IXa shows that these compounds adopt a similar binding mode to that previously observed with pyrazole inhibitors in the factor Xa active site both with regard to how the inhibitor binds and the position of Tyr99.
Keywords :
Pyrazole.* Corresponding author. Tel.: +1 609 818 5332 , fax: +1 609 8183450 , e-mail: joanne.smallheer@bms.com , Factor IXa , factor Xa
