Synthesis of 2-Phenylthiazolidine Derivatives as Cardiotonic Agents. I. 2-Phenylthiazolidine-3-thiocarboxamides(Medicinal Chemistry,Chemical)
スポンサーリンク
概要
- 論文の詳細を見る
A series of novel 2-phenylthiazolidine-3-thiocarboxamides (II) was synthesized and tested for positive inotropic activity in the isolated guinea pig heart and in anesthetized dogs. Reaction of the benzaldehydes (VI, XI, XIV and XV) with cysteamine followed by treatment with isothiocyanates readily gave II. Structure-activity relationships were investigated by varying the structural parameters. N-Methyl-2-phenylthiazolidine-3-thiocarboxamides having an ortho substituent such as a Me or OMe group exhibited significant positive inotropic action, which was not blocked by propranolol. Among the various ortho-alkoxyphenyl derivatives synthesized, the 2-(2-(3-(4-phenylpiperazino)propoxy)phenyl) derivative (I_<67>) was found to exhibit more potent and longerlasting activity than amrinone without any significant effect on heart rate or blood pressure.
- 社団法人日本薬学会の論文
- 1987-05-25
著者
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武田 幹男
Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.,
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名手 博行
Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.
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関根 康雄
Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.
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本間 靖
Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.
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和田 博
Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.
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矢花 秀雄
Biological Research Laboratory, Tanabe Seiyaku Co., Ltd.
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関根 康雄
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.
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和田 博
Organic Chemistry Research Laboratory Tanabe Seiyaku Co . Ltd.
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NATE HIROYUKI
Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.
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NAKAI HIDEO
Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.
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NAGAO TAKU
Biological Research Laboratory, Tanabe Seiyaku Co., Ltd.
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仲井 英雄
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.
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関根 康雄
タナベセイヤク
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長尾 拓
Department Of Toxicology And Pharmacology Faculty Of Pharmaceutical Sciences University Of Tokyo
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仲井 英夫
田辺製薬研
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中井 英雄
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.
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名手 博行
タナベセイヤク
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Nagao Taku
Biological Research Laboratory Tanabe Seiyaku Co. Ltd.
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Nakai H
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.
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Nakai Hideo
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.
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Nate H
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.
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Nate Hiroyuki
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.
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矢花 秀雄
Department Of Toxicology And Pharmacology Faculty Of Pharmaceutical Sciences University Of Tokyo
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本間 靖
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.
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武田 幹男
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.
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NAGAO Taku
Biological Research Laboratories, Tauabe Seiyaku Co., Ltd.
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