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Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 May 01; Vol. 18 (9), pp. 2845-9. Date of Electronic Publication: 2008 Apr 08. - Publication Year :
- 2008
-
Abstract
- Introduction of the phenyl piperidinone and phenyl pyridinone P4 moieties in the anthranilamide scaffold led to potent, selective, and orally bioavailable inhibitors of factor Xa. Anthranilamide 28 displayed comparable efficacy to apixaban in the rabbit arteriovenous-shunt (AV) thrombosis model.
- Subjects :
- Administration, Oral
Animals
Arteriovenous Shunt, Surgical
Binding Sites
Biological Availability
Models, Animal
Rabbits
Structure-Activity Relationship
Thrombosis etiology
Antithrombin III administration & dosage
Antithrombin III chemical synthesis
Antithrombin III pharmacokinetics
Piperidines chemistry
Pyridones chemistry
Serine Proteinase Inhibitors administration & dosage
Serine Proteinase Inhibitors chemical synthesis
Serine Proteinase Inhibitors pharmacokinetics
Thrombosis drug therapy
ortho-Aminobenzoates chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18424044
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.03.092