Synthesis of Thiazolidine-2-thione Derivatives and Evaluation of Their Hepatoprotective Effects
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概要
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A series of N-(mercaptoalkyl)thiazolidine-2-thiones and their derivatives were synthesized and evaluated for hepatoprotective activities against Propionibacterium acnes-lipopolysaccharide (P. acnes-LPS)-induced liver injury in mice and in vitro lipid peroxide (LPO) formation in rat liver microsomes. Reaction of N-(p-methoxybenzylthioalkyl)cysteine methyl ester (11) with 1,1'-thiocarbonyldiimidazole followed by deprotection gave the corresponding thiazolidene-2-thione derivatives. Among the compounds synthesized, 1a and 2a showed the most potent hepato-protective activities against P. acnes-LPS-induced liver injury. Compounds 1a-f and 4 inhibited LPO formation in vitro. Compounds 1a and 2a were chosen for further pharmacological evaluations.
- 公益社団法人日本薬学会の論文
- 1993-05-15
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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太田 淳稔
参天製薬(株)眼科研究所
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米田 耕治
Central Research Laboratories, Santen Pharmaceutical Co., Ltd.,
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米田 耕治
Central Research Laboratories Santen Pharmaceutical Co. Ltd.
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