Synthetic Studies on Selective Type 4 Phosphodiesterase (PDE 4) Inhibitors. 1. Structure-Activity Relationships and Pharmacological Evaluation of 1,8-Naphthyridin-2(1H)-one Derivatives
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概要
- 論文の詳細を見る
In order to develop novel and orally active phosphodiesterase (PDE) 4 inhibitors, random screening was performed using our chemical library to find YM-10335 possessing the 1,8-naphthyridin-2(1H)-one skeleton which is a completely different structure from rolipram. In this report, the syntheses and structure-activity relationships of the YM-10335 derivatives were described. Some compounds showed selective inhibitory activities for PDE 4 derived from human peripheral blood cells and no effect on the other PDE types (1, 2, 3, 5). The inhibition of the tumor necrosis factor-alpha (TNF-α) release in vitro and the carrageenan-induced pleurisy in rats were also described.
- 公益社団法人日本薬学会の論文
- 2002-08-01
著者
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Iwata M
Institute For Drug Discovery Reserch Yamanouchi Pharmaceutical Co. Ltd.
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OKAMOTO Yoshinori
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,
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Iwata Masahiro
Institute For Drug Discovery Reserch Yamanouchi Pharmaceutical Co. Ltd.
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Niwa A
Institute For Drug Development Research Yamanouchi Pharmaceutical Co. Ltd.
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Okamoto Y
Chemistry Research Laboratories Astellas Pharmaceutical Inc.
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TAKAYAMA Kazuhisa
Institute for Drug Discovery Reserch, Yamanouchi Pharmaceutical Co., Ltd.
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HISAMICHI Hiroyuki
Institute for Drug Discovery Reserch, Yamanouchi Pharmaceutical Co., Ltd.
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AOKI Motonori
Institute for Drug Discovery Reserch, Yamanouchi Pharmaceutical Co., Ltd.
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NIWA Akira
Institute for Drug Development Research, Yamanouchi Pharmaceutical Co., Ltd.
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Aoki Motonori
Institute For Drug Discovery Reserch Yamanouchi Pharmaceutical Co. Ltd.
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Aoki Motonori
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Niwa Akira
Institute For Drug Development Research Yamanouchi Pharmaceutical Co. Ltd.
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Takayama Kazuhisa
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Takayama Kazuhisa
Institute For Drug Discovery Reserch Yamanouchi Pharmaceutical Co. Ltd.
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Hisamichi Hiroyuki
Institute For Drug Discovery Reserch Yamanouchi Pharmaceutical Co. Ltd.
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