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Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2002 Oct 21; Vol. 12 (20), pp. 2907-11. - Publication Year :
- 2002
-
Abstract
- Guided by molecular modeling, docking experiments, and available X-ray crystal structure data on the serine protease Factor VIIa and thrombin, a series of indolizidinone derivatives was designed and synthesized having diverse functionality at the P1, P2, and P3 sites.
- Subjects :
- Crystallography, X-Ray
Drug Design
Fibrinolysin chemistry
Humans
Models, Molecular
Molecular Conformation
Spectrometry, Mass, Electrospray Ionization
Structure-Activity Relationship
Factor VIIa antagonists & inhibitors
Factor VIIa chemistry
Indolizines chemical synthesis
Indolizines pharmacology
Thrombin antagonists & inhibitors
Thrombin chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 12
- Issue :
- 20
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 12270173
- Full Text :
- https://doi.org/10.1016/s0960-894x(02)00612-1