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Synthesis and biological activity of novel 1,4-diazepane derivatives as factor Xa inhibitor with potent anticoagulant and antithrombotic activity.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2004 May 01; Vol. 12 (9), pp. 2179-91. - Publication Year :
- 2004
-
Abstract
- Factor Xa (fXa) is a serine protease involved in the coagulation cascade, which has received great interest as a potential target for the development of new antithrombotic drugs. Herein we report a novel series of fXa inhibitors in which the 1,4-diazepane moiety was designed to interact with the S4 aryl-binding domain of the fXa active site. Compound 13 (YM-96765) showed potent fXa inhibitory activity (IC(50) = 6.8 nM) and effective antithrombotic activity without prolonging bleeding time.
Details
- Language :
- English
- ISSN :
- 0968-0896
- Volume :
- 12
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 15080918
- Full Text :
- https://doi.org/10.1016/j.bmc.2004.02.022