Cinnamylindoline Derivatives: Synthesis and Factor Xa (FXa) Inhibitory Activities
-
- Noguchi Tetsuji
- Medicinal Chemistry Research Laboratories II, Daiichi Sankyo Co., Ltd.
-
- Tanaka Naoki
- Medicinal Chemistry Research Laboratories I, Daiichi Sankyo Co., Ltd.
-
- Nishimata Toyoki
- Medicinal Chemistry Research Laboratories I, Daiichi Sankyo Co., Ltd.
-
- Goto Riki
- Medicinal Chemistry Research Laboratories I, Daiichi Sankyo Co., Ltd.
-
- Hayakawa Miho
- Medicinal Chemistry Research Laboratories II, Daiichi Sankyo Co., Ltd.
-
- Sugidachi Atsuhiro
- Biological Research Laboratories II, Daiichi Sankyo Co., Ltd.
-
- Ogawa Taketoshi
- Biological Research Laboratories I, Daiichi Sankyo Co., Ltd.
-
- Asai Fumitoshi
- Biological Research Laboratories II, Daiichi Sankyo Co., Ltd.
-
- Fujimoto Koichi
- Medicinal Chemistry Research Laboratories I, Daiichi Sankyo Co., Ltd.
この論文をさがす
抄録
A series of cinnamylindoline derivatives were synthesized, and their factor Xa (FXa) inhibitory activities and selectivity over trypsin were evaluated. Among them, some novel derivatives showed potent FXa inhibitory activities and good selectivity over trypsin. Especially, (E)-2-{5-[1-(acetimidoyl)piperidin-4-yloxy]-2-[2-(5-amidino-2-hydroxyphenyl)ethen-1-yl]indolin-1-ylsulfonyl}acetic acid (22f) having 2-hydroxycinnamyl moiety exhibited the most potent FXa inhibitory activity in vitro. Furthermore, 22f also exhibited potent anticoagulant activities in vitro.
収録刊行物
-
- CHEMICAL & PHARMACEUTICAL BULLETIN
-
CHEMICAL & PHARMACEUTICAL BULLETIN 55 (10), 1494-1504, 2007
公益社団法人 日本薬学会
- Tweet
詳細情報 詳細情報について
-
- CRID
- 1390001204170911232
-
- NII論文ID
- 110006404699
-
- NII書誌ID
- AA00602100
-
- ISSN
- 13475223
- 00092363
-
- NDL書誌ID
- 8918999
-
- 本文言語コード
- en
-
- データソース種別
-
- JaLC
- NDL
- Crossref
- CiNii Articles
-
- 抄録ライセンスフラグ
- 使用不可