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Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties
- Source :
- Bioorganicmedicinal chemistry letters. 16(21)
- Publication Year :
- 2006
-
Abstract
- The bicyclic dihydropyrazolopyridinone scaffold allowed for incorporation of multiple P1 moieties with subnanomolar binding affinities for blood coagulation factor Xa. The compound 3-[6-(2′-dimethylaminomethyl-biphenyl-4-yl)-7-oxo-3-trifluoro-methyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridine-l-yl]-benzamide 6d shows good fXa potency, selectivity, in vivo efficacy and oral bioavailability. Compound 6d was selected for further pre-clinical evaluations.
- Subjects :
- Tertiary amine
Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Administration, Oral
Pharmacology
Biochemistry
Thrombin
Fibrinolytic Agents
In vivo
Drug Discovery
Pyrazolopyridine
medicine
Potency
Humans
Molecular Biology
Bicyclic molecule
biology
Chemistry
Organic Chemistry
Bioavailability
Treatment Outcome
Enzyme inhibitor
Benzamides
biology.protein
Molecular Medicine
medicine.drug
Factor Xa Inhibitors
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 16
- Issue :
- 21
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....c52dd494e3a6592d7d228d7e88686de2