Preparations of 5-Alkylmethylidene-3-carboxymethylrhodanine Derivatives and Their Aldose Reductase Inhibitory Activity

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概要

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• Reactions of 3-carboxymethylrhodanine (1) with aldehydes (2a-u) afforded stereoselectively the 5-monoalkymethylidene-3-carboxymethylrhodanines (3a-u). The configuration of the 5-monoalkylmethylidene-3-carboxymethylrhodanine (3k) were examined by X-ray structure analysis and confirmed to be Z-configuration. The stereoselective reaction path was discussed. Several 5-dialkylmethylidene-3-carboxymethylrhodanines (15a-f) and alkyl-amino derivatives of 3-carboxymethylrhodanines (18a-o) were also prepared.These products were evaluated for aldose reductase-inhibitory potency and half of them exhibited valuable inhibitory potency.

• 公益社団法人日本薬学会の論文
• 1990-07-25

著者

• 宮原 一元

  Faculty of Pharmaceutical Sciences, Setsunan University

• 宮原 一元

  Faculty Of Pharmaceutical Sciences Setsunan University

• 大石 義孝

  Central Research Institute, Kaken Pharmaceutical Co., Ltd.,

• 大石 義孝

  Central Research Institute Kaken Pharmaceutical Co. Ltd.

• 矢嶋 基之

  Central Research Institute Kaken Pharmaceutical Co. Ltd.

• 永原 美知子

  Central Research Institute, Kaken Pharmaceutical Co., Ltd.,

• 向井 輝夫

  Central Research Institute, Kaken Pharmaceutical Co., Ltd.,

• 梶川 憲雄

  Central Research Institute, Kaken Pharmaceutical Co., Ltd.,

• 高野 常広

  Faculty of Pharmaceutical Science, Setsunan University

• 梶川 憲男

  Central Research Institute, Kaken Pharmaceutical Co., Ltd.,

• 梶川 憲男

  Central Research Institute Kaken Pharmaceutical Co. Ltd.

• 高野 常広

  Faculty Of Pharmaceutical Science Setsunan University

• 永原 美知子

  Central Research Institute Kaken Pharmaceutical Co. Ltd.

• 向井 輝夫

  Central Research Institute Kaken Pharmaceutical Co. Ltd.

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