Preparation of meta-amidino- N, N-disubstituted anilines as potent inhibitors of coagulation factor Xa

The serine protease factor Xa is a critical enzyme in the blood coagulation cascade. Recently, the inhibition of factor Xa has begun to emerge as an attractive strategy for the discovery of novel antithrombotic agents. Here we describe a series of meta-amidino- N, N-disubstituted anilines as structu...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-11, Vol.8 (22), p.3143-3148
Main Authors: Fevig, John M., Cacciola, Joseph, Alexander, Richard S., Knabb, Robert M., Lam, Gilbert N., Wong, Pancras C., Wexler, Ruth R.
Format: Article
Language:English
Subjects:
Aniline Compounds - chemical synthesis
Aniline Compounds - pharmacology
Animals
Biological and medical sciences
Blood. Blood coagulation. Reticuloendothelial system
Factor Xa Inhibitors
Fibrinolytic Agents - chemical synthesis
Fibrinolytic Agents - pharmacology
Humans
Medical sciences
Pharmacology. Drug treatments
Rabbits
Structure-Activity Relationship
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Summary:The serine protease factor Xa is a critical enzyme in the blood coagulation cascade. Recently, the inhibition of factor Xa has begun to emerge as an attractive strategy for the discovery of novel antithrombotic agents. Here we describe a series of meta-amidino- N, N-disubstituted anilines as structurally simple and very potent inhibitors of factor Xa. The serine protease factor Xa is a critical enzyme in the blood coagulation cascade. Recently, the inhibition of factor Xa has begun to emerge as an attractive strategy for the discovery of novel antithrombotic agents. Here we describe a series of meta-amidino- N, N-disubstituted anilines as structurally simple and very potent inhibitors of factor Xa.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00574-5