(−)-Cercosporamide derivatives as novel antihyperglycemic agents

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• 作者：Akihiro Furukawa ; Tsuyoshi Arita ; Susumu Satoh ; Kazushi Araki ; Masanori Kuroha ; Jun Ohsumi
• 关键词：(− ; )-Cercosporamide ; Antihyperglycemic agent
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：1 February 2009
• 年：2009
• 卷：19
• 期：3
• 页码：724-726
• 全文大小：150 K

文摘

In our exploratory campaign for an antihyperglycemic agent with a novel mechanism of action, (−)-Cercosporamide 1, which is known as an antifungal agent, showed a potent plasma glucose lowering effect in hyperglycemic KK/Ta mice. The trouble was that it was accompanied by a decrease in food intake and a loss of body weight. We synthesized some (−)-Cercosporamide derivatives and succeeded to separate these actions. N,O-ketal type derivatives, especially compound 10, had the most potent plasma glucose lowering effect without affecting the food consumption or body weight.