Cinnamyl Derivatives : Synthesis and Factor Xa (FXa) Inhibitory Activities
スポンサーリンク
概要
- 論文の詳細を見る
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 IC_<50> values of less than 10nM in vitro. These compounds also showed potent anticoagulant activities both in vitro and ex vivo. Furthermore, these compounds exhibited no lethal toxicity (30mg/kg,i.v.).
- 公益社団法人日本薬学会の論文
- 2008-06-01
著者
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Tanaka N
Department Of Pharmacology School Of Pharmaceutical Sciences Mukogawa Women's University
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Tanaka Naoko
武庫川女子大学 薬学部薬理学
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Tanaka Naoki
Medical ProteoScope Co., Ltd.
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中西 務
Faculty Of Pharmaceutical Sciences Setsunan University
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Tanaka N
School Of Pharmaceutical Sciences Mukogawa Women S University
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Ogawa T
R & D Division Daiichi Sankyo Co. Ltd.
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NOGUCHI Tetsuji
Medicinal Chemistry Research Laboratories II, Daiichi Sankyo Co., Ltd.
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NISHIMATA Toyoki
Medicinal Chemistry Research Laboratories I, Daiichi Sankyo Co., Ltd.
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GOTO Riki
Medicinal Chemistry Research Laboratories I, Daiichi Sankyo Co., Ltd.
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HAYAKAWA Miho
Medicinal Chemistry Research Laboratories II, Daiichi Sankyo Co., Ltd.
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SUGIDACHI Atsuhiro
Biological Research Laboratories II, Daiichi Sankyo Co., Ltd.
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OGAWA Taketoshi
Biological Research Laboratories I, Daiichi Sankyo Co., Ltd.
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ASAI Fumitoshi
Biological Research Laboratories II, Daiichi Sankyo Co., Ltd.
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FUJIMOTO Koichi
Medicinal Chemistry Research Laboratories I, Daiichi Sankyo Co., Ltd.
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Goto R
R & D Division Daiichi Sankyo Co. Ltd.
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Hayakawa Miho
R & D Division Daiichi Sankyo Co. Ltd.
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Asai Fumitoshi
R & D Division Daiichi Sankyo Co. Ltd.
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Fujimoto K
R & D Division Daiichi Sankyo Co. Ltd.
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Noguchi Tetsuji
R & D Division Daiichi Sankyo Co. Ltd.
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Sugidachi Atsuhiro
R & D Division Daiichi Sankyo Co. Ltd.
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Nishimata Toyoki
R & D Division Daiichi Sankyo Co. Ltd.
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