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Structure–activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties
- Source :
- Bioorganic & Medicinal Chemistry Letters. 18:2845-2849
- Publication Year :
- 2008
- Publisher :
- Elsevier BV, 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 :
- Serine Proteinase Inhibitors
Molecular model
medicine.drug_mechanism_of_action
Pyridones
Stereochemistry
medicine.drug_class
Antithrombin III
Clinical Biochemistry
Factor Xa Inhibitor
Administration, Oral
Biological Availability
Pharmaceutical Science
Carboxamide
Biochemistry
Structure-Activity Relationship
chemistry.chemical_compound
Arteriovenous Shunt, Surgical
Piperidines
Drug Discovery
Hydrolase
medicine
Animals
Structure–activity relationship
ortho-Aminobenzoates
Molecular Biology
chemistry.chemical_classification
Binding Sites
biology
Organic Chemistry
Thrombosis
Enzyme
chemistry
Enzyme inhibitor
Models, Animal
Lactam
biology.protein
Molecular Medicine
Rabbits
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 18
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....71f0e123723f0355168a127b067954db