書誌事項
- タイトル別名
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- Angiotensin II Receptor Antagonists : Candesartan Cilexetil
- アンジオテンシン 2 ジュヨウタイ キッコウヤク カンデサルタン シレキセチル ノ ソウセイ
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説明
Blockade of the action of angiotensin II (AII) has long been a target for the development of novel antihypertensive agents. We recently discovered a novel class of potent nonpeptide AII receptor antagonists, benzimidazole-7-carboxylic acids including candesartan. Candesartan is a highly potent and insurmountable AII type-1 receptor (AT1)-selective antagonist. Structure-activity relationship (SAR) studies revealed that the adjacent arrangement of a lipophilic substituent, a tetrazolylbiphenylmethyl moiety and a carboxyl group was the important structural requirement for potent AII antagonistic activity. Especially, the presence of a carboxyl group at the 7-position was found to be essential for insurmountable antagonism. To improve bioavailability of candesartan, chemical modification was examined to yield candesartan cilexetil, a prodrug of candesartan. Candesartan cilexetil is a potent and long-acting blocker that, when given once a day to patients, provides effective 24 hr blood pressure control.
収録刊行物
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- 薬学雑誌
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薬学雑誌 120 (12), 1261-1275, 2000
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
- 1390282681130425344
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- NII論文ID
- 110003648783
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- NII書誌ID
- AN00284903
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- ISSN
- 13475231
- 00316903
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- NDL書誌ID
- 5600945
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- データソース種別
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- JaLC
- NDL
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