Synthesis and Structure-Activity Relationships of Novel Phenylcyanoguanidine Derivatives as Potassium Channel Openers.
書誌事項
- タイトル別名
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- Synthesis and Structure-Activity Relati
- 公開日
- 1996
- 資源種別
- journal article
- DOI
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- 10.1248/cpb.44.2042
- 公開者
- 公益社団法人 日本薬学会
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説明
3, 5-Di-substituted phenylcyanoguanidine derivatives with halogen, cyano, and/or nitro groups at the 3- and 5-positions of the benzene ring exhibited very strong smooth muscle relaxation activity in vitro, as compared to pinacidil. Among them, N-(3-chloro-5-cyanophenyl)-N'-cyano-N"-tert-pentylguanidine (5s) showed 27-fold more potent activity than pinacidil, and exhibited a stronger and more lasting antihypertensive effect than pinancidil by oral administration to spontaneously hypertensive rats. We propose a new pharmacophore model in which the essential factors for binding to the potassium channel are an NH and a bulky alkyl group.
収録刊行物
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- ＣＨＥＭＩＣＡＬ ＆ ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＢＵＬＬＥＴＩＮ
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ＣＨＥＭＩＣＡＬ ＆ ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＢＵＬＬＥＴＩＮ 44 (11), 2042-2050, 1996
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
- 1390282679140702592
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- NII論文ID
- 130003947059
- 110003631812
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 4079999
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- PubMed
- 8945769
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- 本文言語コード
- en
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- 資料種別
- journal article
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- データソース種別
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- JaLC
- NDLサーチ
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
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