SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.
Bioorg Med Chem Lett
; 14(21): 5263-7, 2004 Nov 01.
Article
in En
| MEDLINE
| ID: mdl-15454208
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.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Pyrazoles
/
Benzimidazoles
/
Factor IXa
/
Factor Xa
/
Factor Xa Inhibitors
Type of study:
Prognostic_studies
Limits:
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2004
Document type:
Article
Affiliation country:
United States