Inhibitors of Adhesion Molecules Expression; The Synthesis and Pharmacological Properties of 10H-Pyrazino[2,3-b][1,4]benzothiazine Derivatives.
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- Kaneko Toshihiko
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- Clark Richard S. J.
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- Ohi Norihito
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- Kawahara Tetsuya
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- Akamatsu Hiroshi
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- Ozaki Fumihiro
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- Kamada Atsushi
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- Okano Kazuo
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- Yokohama Hiromitsu
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- Muramoto Kenzo
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- Ohkuro Masayoshi
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- Takenaka Osamu
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- Kobayashi Seiichi
- Eisai Research Institute of Boston, Inc.
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抄録
During a search for novel, orally-active inhibitors of upregulation of adhesion molecules such as intercellular adhesion molecule-1 (ICAM-1), we found a new series of 10H-pyrazino[2,3-b][1,4]benzothiazine derivatives to be potent ICAM-1 inhibitors. Of these compounds, N-[1-(10H-Pyrazino[2,3-b][1,4]benzothiazin-8-ylmethyl)piperidin-4-yl]-N′,N′-dimethylsulfamide 7p showed the potent oral inhibitory activities against neutrophil migration in a murine interleukin-1 (IL-1) induced paw inflammation model. The synthesis and structure–activity relationships of these amide derivatives are described.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 50 (7), 922-929, 2002
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679138902528
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- NII論文ID
- 110003616274
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- NII書誌ID
- AA00602100
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- COI
- 1:CAS:528:DC%2BD38XlvVCht7s%3D
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 6262682
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- PubMed
- 12130850
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可