Abstract
A series of novel 2,7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds 1 and 2 (JTV-803) exhibited potent inhibitory activity against FXa and good selectivity with respect to other serine proteases (thrombin, plasmin, and trypsin). In addition, compound 2 exhibited potent anti-FXa activity after intravenous and oral administration to cynomolgus monkey, and showed a dose-dependent antithrombotic effect in a rat model of venous thrombosis.
Original language | English |
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Pages (from-to) | 185-189 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 15 |
Issue number | 1 |
DOIs | |
Publication status | Published - 2005 Jan 3 |
Keywords
- Antithrombotic effect on venous thrombosis in rats
- Inhibition of human FXa
- JTV-803
- Potent and selective factor Xa (FXa) inhibitor
- Tetrahydroisoquinoline derivatives
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry