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Bioorg Med Chem Lett. 2004 Nov 1;14(21):5263-7.

SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.

Author information

1
Bristol-Myers Squibb Company, PO Box 5400, Princeton, NJ 08543-5400, USA. joanne.smallheer@bms.com

Abstract

Modifications to the P4 moiety and pyrazole C3 substituent of factor Xa inhibitor SN-429 provided several new compounds, which are 5-10nM 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.

PMID:
15454208
DOI:
10.1016/j.bmcl.2004.08.034
[Indexed for MEDLINE]

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