1,4 : 3,6-Dianhydrohexitol Nitrate Derivatives. I. Synthesis and Antianginal Activity of Alkylpiperazine Derivatives
スポンサーリンク
概要
- 論文の詳細を見る
A series of 5-deoxy-5-(4-substituted piperazin-1-yl)-1,4 : 3,6-dianhydro-L-iditol 2-nitrates was prepared and evaluated for oral anti-ischemic activities. Inhibition of lysine-vasopressin-induced T-wave elevation in the electrocardiogram (ECG) of rats (angina pectoris model) served as a primary assay. Optimum activity was observed for the compounds with the aryl-heteroatom (O, S, or N)-propyl group. Among them, the phenylthiopropyl-substituted compound 13 exhibited the most potent activity. Furthermore, intraduodenal administration (i.d.) of 13 tended to decrease left ventricular end-diastolic pressure (LVEDP) in a propranolol-induced heart failure model (dogs) and showed a potent protective effect against reperfusion arrhythmia in rats. Thus, 13 (KF 14124) is under further study as an orally active nitrate.
- 社団法人日本薬学会の論文
- 1993-06-15
著者
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池田 淳一
Pharmaceutical Research Laboratories Kyowa Hakko Kogyo Co. Ltd.
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黒田 武志
Pharmaceutical Research Laboratories Kyowa Hakko Kogyo Co. Ltd.
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林 裕晃
Pharmaceutical Research Laboratories Kyowa Hakko Kogyo Co. Ltd.
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鈴木 文夫
Pharmaceutical Research Laboratories Kyowa Hakko Kogyo Co. Ltd.
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久保 和博
Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co., Ltd.,
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佐野 智行
Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co., Ltd.,
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久保 和博
Pharmaceutical Research Laboratories Fuji Kyowa Hakko Kogyo Co. Ltd.
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佐野 智行
Pharmaceutical Research Laboratories Kyowa Hakko Kogyo Co. Ltd.
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