Synthesis and Activity of a Metabolite of (S)-6-Amino-5-(6-hydroxy-2, 5, 7, 8-tetramethylchroman-2-carboxamido)-3-methyl-1-phenyl-2, 4-(1H, 3H)-pyrimidinedione (CX-659S)

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概要

• 論文の詳細を見る

• CX-659S (1) [(S)-6-amino-5-(6-hydroxy-2, 5, 7, 8-tetrametylchroman-2-carboxamido)-3-methyl-1-phenyl-2, 4-(1H, 3H)-pyrimidinedione], has been developed as a new type anti-inflammatory agent for the treatment of dermatitis. The structure of a major metabolite of CX-659S was determined as (S)-6-amino-5-[2-hydroxy-2-methyl-4-(2, 4, 5-trimethyl-3, 6-dioxo-1, 4-cyclohexadienyl)butanamide]-3-methyl-1-phenyl-2, 4-(1H, 3H)-pyrimidinedione (2) by direct comparison with the synthesized authentic compound. The anti-inflammatory activity of 2 was equipotent with that of 1 on the contact hypersensitivity reaction (CHR) induced by picryl chloride (PC) in mice, suggesting that compound 2 contributes, at least in part, to the anti-inflammatory activity of CX-659S.

• 社団法人日本薬学会の論文
• 2002-10-01

著者

• Tsuchiya M

  Pharmaceuticals And Biotechnology Laboratory Japan Energy Corporation

• ISOBE Yoshiaki

  Pharmaceuticals and Biotechnology Laboratory, Japan Energy Corporation

• TOBE Masanori

  Pharmaceuticals and Biotechnology Laboratory, Japan Energy Corporation

• TAKAHASHI Osamu

  Pharmaceuticals and Biotechnology Laboratory, Japan Energy Corporation

• GOTO Yuso

  Pharmaceuticals and Biotechnology Laboratory, Japan Energy Corporation

• INOUE Yoshifumi

  Pharmaceuticals and Biotechnology Laboratory, Japan Energy Corporation

• OBARA Fumihiro

  Pharmaceuticals and Biotechnology Laboratory, Japan Energy Corporation

• TSUCHIYA Masami

  Pharmaceuticals and Biotechnology Laboratory, Japan Energy Corporation

• HAYASHI Hideya

  Pharmaceuticals and Biotechnology Laboratory, Japan Energy Corporation

• Hayashi H

  Univ. Tokyo Tokyo Jpn

• Goto Y

  Pharmaceuticals & Biotechnology Laboratory Japan Energy Corporation

• Tobe M

  Sumitomo Pharmaceuticals Co. Ltd. Osaka Jpn

• Obara Fumihiro

  Pharmaceuticals And Biotechnology Laboratory Japan Energy Corporation

• Hayashi H

  Drug Research Division Dainippon Sumitomo Pharma Co. Ltd.

• Hayashi Hideya

  Pharmaceuticals And Biotechnology Laboratory Japan Energy Corporation

• Hayashi H

  Pharmaceuticals & Biotechnology Laboratory Japan Energy Corporation

• Hayashi Hideya

  Pharmaceuticals & Biotechnology Laboratory Japan Energy Corporation

• Isobe Y

  Research Division Discovery Research Laboratories Ii Sumitomo Pharmaceuticals Co. Ltd.

• Isobe Yoshiaki

  Pharmaceuticals And Biotechnology Laboratory Japan Energy Corporation

• Isobe Y

  Sumitomo Pharmaceuticals Co. Ltd. Osaka Jpn

• Isobe Y

  Pharmaceuticals And Biotechnology Laboratory Japan Energy Corporation

• 五十部 穣

  Research Center Sumitomo Pharmaceuticals Co. Ltd.

• Tsuchiya Masami

  Pharmaceuticals And Biotechnology Laboratory Japan Energy Corporation

• Goto Yuso

  Pharmaceuticals & Biotechnology Laboratory Japan Energy Corporation

• Tobe Masanori

  Pharmaceuticals And Biotechnology Laboratory Japan Energy Corporation

• Tsuchiya M

  Chiba Univ. Chiba Jpn

• 土谷 満美子

  Faculty Of Pharmaceutical Sciences Toyama Medical And Pharmaceutical University

• Takahashi Osamu

  Pharmaceuticals And Biotechnology Laboratory Japan Energy Corporation

• Isobe Yoshiaki

  Pharmaceuticals & Biotechnology Laboratory Japan Energy Corporation

• Takahashi Osamu

  Pharmaceuticals & Biotechnology Laboratory Japan Enery Corporation

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