Title of article
SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
5
From page
5263
To page
5267
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
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794967
Link To Document