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Design and synthesis of glycolic and mandelic acid derivatives as factor Xa inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2001 Sep 03; Vol. 11 (17), pp. 2279-82. - Publication Year :
- 2001
-
Abstract
- A series of glycolic and mandelic acid derivatives was synthesized and investigated for their factor Xa inhibitory activity. These analogues are highly potent and selective inhibitors against fXa. In a rabbit deep vein thrombosis model, compound 26 showed significant antithrombotic effects (81% inhibition of thrombus formation) at 1.1 microM plasma concentration following intravenous administration.
- Subjects :
- Amidines chemical synthesis
Animals
Biological Availability
Blood Coagulation Tests
Drug Design
Drug Evaluation, Preclinical methods
Fibrinolysin antagonists & inhibitors
Inhibitory Concentration 50
Injections, Intravenous
Phenylacetates chemical synthesis
Rabbits
Rats
Rats, Sprague-Dawley
Serine Proteinase Inhibitors chemical synthesis
Structure-Activity Relationship
Venous Thrombosis drug therapy
Acetanilides
Amidines chemistry
Amidines pharmacology
Factor Xa Inhibitors
Mandelic Acids chemistry
Phenylacetates chemistry
Phenylacetates pharmacology
Serine Proteinase Inhibitors chemistry
Serine Proteinase Inhibitors pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 11
- Issue :
- 17
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 11527714
- Full Text :
- https://doi.org/10.1016/s0960-894x(01)00447-4