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Investigation of factor Xa inhibitors containing non-amidine S1 elements.
Franciskovich, Jeffry B; Masters, John J; Tinsley, Jennifer M; Craft, Trelia J; Froelich, Larry L; Gifford-Moore, Donetta S; Klimkowski, Valentine J; Smallwood, Jeffrey K; Smith, Gerald F; Smith, Tommy; Towner, Richard R; Weir, Leonard C; Wiley, Michael R.
Bioorg Med Chem Lett ; 15(21): 4838-41, 2005 Nov 01.
Article in English | MEDLINE | ID: mdl-16140530

ABSTRACT

Several non-amidino S1 derivatives of the 1,2-diaminobenzene-based scaffold (4) were synthesized and evaluated for their ability to bind to the active site and inhibit the human protease factor Xa. A subset of these compounds were also evaluated for their anticoagulant effects in human plasma as measured by prothrombin time (PT).


Subject(s)
Anticoagulants/chemical synthesis , Benzene Derivatives/chemical synthesis , Factor Xa Inhibitors , Anticoagulants/pharmacology , Benzene Derivatives/pharmacology , Binding Sites , Blood Coagulation/drug effects , Factor Xa/metabolism , Humans , Models, Molecular , Protease Inhibitors/chemical synthesis , Protease Inhibitors/pharmacology , Protein Binding , Prothrombin Time , Structure-Activity Relationship
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