Novel trifluoroacetophenone derivatives as malonyl-CoA decarboxylase inhibitors

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• 作者：David M. Wallace ; Masayuki Haramura ; Jie-Fei Cheng ; Thomas Arrhenius ; Alex M. Nadzan
• 关键词：Trifluoroacetyl ; Trifluoroacetophenone ; Malonyl-CoA ; Acetyl-CoA ; Malonyl-CoA decarboxylase ; MCD ; Fatty acid oxidation ; Glucose oxidation
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 February 2007
• 卷：17
• 期：4
• 页码：1127-1130
• 文件大小：150 K

摘要

A series of trifluoroacetophenone derivatives were prepared and evaluated as malonyl-CoA decarboxylase (MCD) inhibitors. Some of the ‘reverse amide’ analogs were found to be potent inhibitors of MCD enzyme activity. The trifluoroacetyl group may interact with the MCD active site as the hydrate in a similar fashion to the hexafluoroisopropanol analogs reported previously. Adding electron-withdrawing groups to the phenyl ring stabilizes the hydrated species and enhances this interaction.