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Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2009 Jul; Vol. 44 (7), pp. 2787-95. Date of Electronic Publication: 2009 Jan 03. - Publication Year :
- 2009
-
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.
- Subjects :
- Aminoquinolines chemistry
Aminoquinolines metabolism
Aminoquinolines pharmacokinetics
Antithrombin III chemistry
Antithrombin III metabolism
Antithrombin III pharmacokinetics
Crystallography, X-Ray
Factor Xa chemistry
Humans
Models, Molecular
Molecular Conformation
Aminoquinolines pharmacology
Antithrombin III pharmacology
Drug Design
Drug Evaluation, Preclinical
Factor Xa metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 44
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 19200624
- Full Text :
- https://doi.org/10.1016/j.ejmech.2008.12.025