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Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with biaryl P4 motifs.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Jan 01; Vol. 18 (1), pp. 23-7. Date of Electronic Publication: 2007 Nov 17. - Publication Year :
- 2008
-
Abstract
- Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating biaryl P4 groups, producing highly potent inhibitors with encouraging oral pharmacokinetic profiles and significant but sub-optimal anticoagulant activities.
- Subjects :
- Animals
Anticoagulants chemistry
Anticoagulants pharmacokinetics
Anticoagulants pharmacology
Drug Design
Male
Models, Molecular
Pyrrolidinones pharmacokinetics
Rats
Rats, Sprague-Dawley
Serine Proteinase Inhibitors pharmacokinetics
Structure-Activity Relationship
Sulfonamides chemistry
Sulfonamides pharmacokinetics
Sulfonamides pharmacology
Factor Xa Inhibitors
Pyrrolidinones chemistry
Pyrrolidinones pharmacology
Serine Proteinase Inhibitors chemistry
Serine Proteinase Inhibitors pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18054228
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.11.023