Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Regular Articles
Discovery of R-142086 as a Factor Xa (FXa) Inhibitor: Syntheses and Structure–Activity Relationships of Cinnamyl Derivatives
Tetsuji Noguchi, Naoki Tanaka, Toyoki Nishimata, Riki Goto, Miho Hayakawa, Atsuhiro Sugidachi, Taketoshi Ogawa, Yoichi Niitsu, Fumitoshi Asai, Tomoko Ishizuka, Koichi Fujimoto
著者情報
キーワード: factor Xa inhibitory activity, cinnamyl derivative, anticoagulant, prodrug, Ames test
ジャーナル フリー

2009 年 57 巻 1 号 p. 22-33

詳細
PDFをダウンロード (492K)
メタデータをダウンロード RIS形式

(EndNote、Reference Manager、ProCite、RefWorksとの互換性あり)

BIB TEX形式

(BibDesk、LaTeXとの互換性あり)

テキスト
メタデータのダウンロード方法
発行機関連絡先
抄録
To develop a novel and effective anticoagulant with potent and selective factor Xa (FXa) inhibitory activity, a new series of cinnamyl derivatives with enhanced lipophilicity and prodrug forms were synthesized and their biological activities were evaluated. As a result, we found that cinnamyl derivative (N-{4-[1-(acetimidoyl)piperidin-4-yloxy]-3-carbamoylphenyl}-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid dihydrochloride (26d, R-142086) with a fluorine atom on the double bond exhibited potent anticoagulant activity and no mutagenic potential. Moreover, orally administered R-142086 exhibited potent anti-FXa activity and anticoagulant activity in dogs.
著者関連情報
© 2009 The Pharmaceutical Society of Japan
前の記事 次の記事
お気に入り & アラート

閲覧履歴
このページを共有する
feedback
 Top
OSZAR »