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Potent and selective TF/FVIIa inhibitors containing a neutral P1 ligand.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2006 Dec 01; Vol. 14 (23), pp. 7688-705. Date of Electronic Publication: 2006 Aug 30. - Publication Year :
- 2006
-
Abstract
- Inhibition of tissue factor/factor VIIa complex (TF/FVIIa) is an attractive strategy for antithrombotic therapies. We began with an investigation of a non-amidine TF/FVIIa inhibitor based on a modification of amidine compound 1. Optimization of the substituents on the P1 phenyl portion of the compound 1 led to a neutral or less basic alternative for the 4-amidinophenyl moiety. By further optimization of the substituents on the central phenyl ring, a highly potent and selective TF/FVIIa inhibitor 17d was discovered.
Details
- Language :
- English
- ISSN :
- 0968-0896
- Volume :
- 14
- Issue :
- 23
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 16942884
- Full Text :
- https://doi.org/10.1016/j.bmc.2006.08.010