4-(Pyrrolidinyl)methoxybenzoic Acid Derivatives as a Potent, Orally Active VLA-4 Antagonist
スポンサーリンク
概要
- 論文の詳細を見る
A novel series of benzoic acid derivatives as VLA-4 antagonists were synthesized. Optimization, focusing on activity and lipophilicity needed for cell permeability, resulted in the identification of 15b and 15e with good activity (IC_<50>=1.6nM each) and moderate lipophilicity (Log D=2.0, 1.8). Furthermore, 15e demonstrated efficacy in murine asthma model by an oral dose of 30mg/kg.
- 公益社団法人日本薬学会の論文
- 2006-11-01
著者
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Horiuchi Takao
Medicinal Chemistry Research Laboratory Daiichi Pharmaceutical Co. Ltd.
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Chiba Jun
Medicinal Chemistry Research Laboratory Daiichi Pharmaceutical Co. Ltd.
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Ochiai Yuichi
Medicinal Chemistry Research Laboratory Daiichi Pharmaceutical Co. Ltd.
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Sugimoto Yuichi
Medicinal Chemistry Research Laboratory Daiichi Pharmaceutical Co. Ltd.
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TAKASHI Tohru
New Product Research Laboratories III, Tokyo R&D Center, Daiichi Pharmaceutical Co., Ltd.
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Yokoyama Mika
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Iimura Shin
Medicinal Chemistry Research Laboratory Daiichi Pharmaceutical Co. Ltd.
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Nakayama Atsushi
Medicinal Chemistry Research Laboratory Daiichi Pharmaceutical Co. Ltd.
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YONEDA Yoshiyuki
Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical, Co., Ltd.
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MURO Fumito
Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical, Co., Ltd.
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OGASAWARA Tomomi
Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical, Co., Ltd.
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TSUBOKAWA Masao
New Product Research Laboratories III, Daiichi Pharmaceutical, Co., Ltd.
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IIGOU Yutaka
New Product Research Laboratories III, Daiichi Pharmaceutical, Co., Ltd.
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TAKAYAMA Gensuke
New Product Research Laboratories III, Daiichi Pharmaceutical, Co., Ltd.
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TAIRA Tomoe
New Product Research Laboratories III, Daiichi Pharmaceutical, Co., Ltd.
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TAKATA Yoshimi
New Product Research Laboratories III, Daiichi Pharmaceutical, Co., Ltd.
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MACHINAGA Nobuo
Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical, Co., Ltd.
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Takashi Tohru
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Taira Tomoe
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Muro Fumito
Medicinal Chemistry Research Laboratory Daiichi Pharmaceutical Co. Ltd.
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Iigou Yutaka
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Takata Yoshimi
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Machinaga Nobuo
Medicinal Chemistry Research Laboratory Daiichi Pharmaceutical Co. Ltd.
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Tsubokawa Masao
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Takayama Gensuke
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Yoneda Yoshiyuki
Medicinal Chemistry Research Laboratory Daiichi Pharmaceutical Co. Ltd.
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Ogasawara Tomomi
Medicinal Chemistry Research Laboratory Daiichi Pharmaceutical Co. Ltd.
関連論文
- Contribution of Translin to Hematopoietic Regeneration after Sublethal Ionizing Irradiation(Highlighted paper selected by Editor-in-chief,Molecular and Cell Biology)
- 4-(Pyrrolidinyl)methoxybenzoic Acid Derivatives as a Potent, Orally Active VLA-4 Antagonist