Synthesis and Pharmacological Activities of Novel Cyclic Disulfide and Cyclic Sulfide Derivatives as Hepatoprotective Agents
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概要
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In order to search for anti-hepatitis drugs, we synthesized a series of eight- and nine-membered cyclic disulfides (1) and six- and seven-membered cyclic sulfides (2) and evaluated them for ability to reduce mortality in the model of acute hepatic failure induced by Propionibacterium acnes-lipopolysaccharide in mice. Compounds 1 were synthesized by oxidative cyclization of the corresponding dithiol derivatives (3) with diethyl bromomalonate or iodine. Compounds 2 were prepared from the methyl esters of 1 by desulfurization with tris(diethylamino)phosphine followed by deprotection. Compounds 1 were generally found to be more active than compounds 2. Compound 1b (SA3443) was found to exhibit potent protective activity. The synthesis and structure-activity relationships are discussed.
- 公益社団法人日本薬学会の論文
- 1993-06-15
著者
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河嶋 洋一
Central Research Laboratories, Santen Pharmaceutical Co., Ltd.,
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河嶋 洋一
参天製薬(株)生産技術部
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河嶋 洋一
Central Research Laboratories Santen Pharmaceutical Co. Ltd.
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太田 淳稔
Central Research Laboratories, Santen Pharmaceutical Co., Ltd.,
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伊藤 研
Central Research Laboratories, Santen Pharmaceutical Co., Ltd.,
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伊藤 研
Central Research Laboratories Santen Pharmaceutical Co. Ltd.
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須原 寛
Central Research Laboratories, Santen Pharmaceutical Co., Ltd.,
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田橋 圭三
Central Research Laboratories, Santen Pharmaceutical Co., Ltd.,
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須原 寛
Central Research Laboratories Santen Pharmaceutical Co. Ltd.
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田橋 圭三
Central Research Laboratories Santen Pharmaceutical Co. Ltd.
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太田 淳稔
参天製薬(株)眼科研究所
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