Abstract
SAR about the B-ring of a series of N(2)-aroyl anthranilamide factor Xa (fXa) inhibitors is described. B-ring o-aminoalkylether and B-ring p-amine probes of the S1' and S4 sites, respectively, afforded picomolar fXa inhibitors that performed well in in vitro anticoagulation assays.
MeSH terms
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Anticoagulants / chemistry
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Antithrombin III / chemical synthesis*
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Antithrombin III / chemistry
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Binding Sites
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Chemistry, Pharmaceutical / methods
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Dose-Response Relationship, Drug
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Drug Design
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Drug Evaluation, Preclinical
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Factor Xa Inhibitors*
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Fluorescent Dyes / chemical synthesis
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Fluorescent Dyes / pharmacology*
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Humans
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Kinetics
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Models, Chemical
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Molecular Conformation
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Structure-Activity Relationship
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ortho-Aminobenzoates / chemical synthesis
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ortho-Aminobenzoates / pharmacology*
Substances
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Anticoagulants
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Factor Xa Inhibitors
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Fluorescent Dyes
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ortho-Aminobenzoates
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Antithrombin III
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anthranilamide