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2. ChemInform Abstract: Cinnamyl Derivatives: Synthesis and Factor Xa (FXa) Inhibitory Activities

Author

Taketoshi Ogawa, Atsuhiro Sugidachi, Fumitoshi Asai, Miho Hayakawa, Riki Goto, Tetsuji Noguchi, Koichi Fujimoto, Toyoki Nishimata, and Naoki Tanaka

Subjects
Acetic acid, chemistry.chemical_compound, chemistry, Stereochemistry, Toxicity, Substituent, Oral anticoagulant, Moiety, General Medicine, Inhibitory postsynaptic potential, In vitro, Ex vivo
Abstract

To develop a potent and oral anticoagulant, a series of compounds with cinnamyl moiety was synthesized and their factor Xa (FXa) inhibitory activities were examined. As a result, some cinnamyl derivatives showed potent FXa inhibitory activities in vitro. Among them, compounds with substituent at the 3-position on the central benzene ring represented by (N-{4-[1-(acetimidoyl)piperidin-4-yloxy]-3-chlorophenyl}-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid dihydrochloride (45b) and (N-{4-[1-(acetimidoyl)piperidin-4-yloxy]-3-carbamoylphenyl}-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid dihydrochloride (45j) exhibited potent FXa inhibitory activities with IC50 values of less than 10 nM in vitro. These compounds also showed potent anticoagulant activities both in vitro and ex vivo. Furthermore, these compounds exhibited no lethal toxicity (30 mg/kg, i.v.).

Published
2008
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