Structure-Activity Relationships of New N-Acylanthranilic Acid Derivatives as Plasminogen Activator Inhibitor-1 Inhibitors
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- Yamaoka Nagahisa
- CT Laboratory, Hamari Chemicals, Ltd.
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- Kodama Hidehiko
- CT Laboratory, Hamari Chemicals, Ltd.
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- Izuhara Yuko
- Center for Translational and Advanced Research, Tohoku University School of Medicine
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- Miyata Toshio
- Center for Translational and Advanced Research, Tohoku University School of Medicine
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- Meguro Kanji
- CT Laboratory, Hamari Chemicals, Ltd.
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Novel anthranilic acid derivatives having substituted N-acyl side chains were designed and synthesized for evaluation as plasminogen activator inhibitor-1 (PAI-1) inhibitors. Compounds with a 4-diphenylmethyl-1-piperazinyl moiety on the acyl side chains in general exhibited potent in vitro PAI-1 inhibitory activity and good pharmacokinetic profiles after oral administration in rats. Compound 16f (TM5275) was identified as a promising candidate for further pharmacological evaluation.
収録刊行物
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- ＣＨＥＭＩＣＡＬ ＆ ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＢＵＬＬＥＴＩＮ
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ＣＨＥＭＩＣＡＬ ＆ ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＢＵＬＬＥＴＩＮ 59 (2), 215-224, 2011
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
- 1390282679149882240
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- NII論文ID
- 130000405518
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 10951877
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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
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可
