Abstract
Starting from a hit identified by focused screening, 3-aminopyrrolidine factor Xa inhibitors were designed. The binding mode as determined by X-ray structural analysis as well as the pharmacokinetic behaviour of selected compounds is discussed.
MeSH terms
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Aminoquinolines / chemistry
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Aminoquinolines / metabolism
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Aminoquinolines / pharmacokinetics
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Aminoquinolines / pharmacology*
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Antithrombin III / chemistry
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Antithrombin III / metabolism
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Antithrombin III / pharmacokinetics
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Antithrombin III / pharmacology*
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Crystallography, X-Ray
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Drug Design*
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Drug Evaluation, Preclinical*
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Factor Xa / chemistry
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Factor Xa / metabolism*
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Humans
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Models, Molecular
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Molecular Conformation
Substances
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Aminoquinolines
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Antithrombin III
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Factor Xa