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Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2014 Aug 01; Vol. 24 (15), pp. 3341-5. Date of Electronic Publication: 2014 Jun 07. - Publication Year :
- 2014
-
Abstract
- In an effort to identify a potential back-up to apixaban (Eliquis®), we explored a series of diversified P4 moieties. Several analogs with substituted gem-dimethyl moieties replacing the terminal lactam of apixaban were identified which demonstrated potent FXa binding affinity (FXa Ki), good human plasma anticoagulant activity (PT EC2x), cell permeability, and oral bioavailability.<br /> (Copyright © 2014 Elsevier Ltd. All rights reserved.)
- Subjects :
- Administration, Oral
Animals
Biological Availability
Cell Membrane Permeability drug effects
Dogs
Dose-Response Relationship, Drug
Factor Xa Inhibitors administration & dosage
Factor Xa Inhibitors chemistry
Humans
Molecular Structure
Pyrazoles administration & dosage
Pyrazoles chemistry
Pyridones administration & dosage
Pyridones chemistry
Structure-Activity Relationship
Factor Xa metabolism
Factor Xa Inhibitors pharmacology
Pyrazoles pharmacology
Pyridones pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 24
- Issue :
- 15
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 24951330
- Full Text :
- https://doi.org/10.1016/j.bmcl.2014.05.101