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Phenyltriazolinones as potent factor Xa inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Feb 15; Vol. 20 (4), pp. 1373-7. Date of Electronic Publication: 2010 Jan 11. - Publication Year :
- 2010
-
Abstract
- We have discovered that phenyltriazolinone is a novel and potent P1 moiety for coagulation factor Xa. X-ray structures of the inhibitors with a phenyltriazolinone in the P1 position revealed that the side chain of Asp189 has reoriented resulting in a novel S1 binding pocket which is larger in size to accommodate the phenyltriazolinone P1 substrate.<br /> (Copyright 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Anticoagulants chemistry
Anticoagulants pharmacology
Crystallography, X-Ray
Humans
Isoxazoles chemistry
Isoxazoles pharmacology
Models, Molecular
Molecular Structure
Pyrazoles chemistry
Pyrazoles pharmacology
Pyridones chemistry
Pyridones pharmacology
Sulfones chemistry
Sulfones pharmacology
Anticoagulants chemical synthesis
Drug Design
Factor Xa Inhibitors
Isoxazoles chemical synthesis
Pyrazoles chemical synthesis
Pyridones chemical synthesis
Sulfones chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 20100660
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.01.011