学術雑誌論文 Synthesis and Biological Evaluation of Piperic Acid Amides as Free Radical Scavengers and α-Glucosidase Inhibitors

高尾, 浩一  ,  宮城, 昂幹  ,  杉田, 義昭

63 ( 5 )  , pp.326 - 333 , 2015-05 , 日本薬学会
ISSN:0009-23631347-5223
NII書誌ID(NCID):AA00602100
内容記述
A series of piperic acid amides (4?24, 29, 30) were synthesized and their 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging and α-glucosidase inhibitory activities were evaluated. Among the synthesized compounds, the amides 11, 13 and 15, which contain o-methoxyphenol, catechol or 5-hydroxyindole moieties, showed potent DPPH free radical scavenging activity (11: EC50 140??M; 13: EC50 28??M; 15: EC50 20??M). The amides 10, 18 and 23 showed higher inhibitory activity of α-glucosidase (10: IC50 21??M; 18: IC50 21??M; 23: IC50 12??M). These data suggest that the hydrophobicity of the conjugated amines is an important determinant of α-glucosidase inhibitory activity. In addition, the amides 13 and 15 showed both potent DPPH free radical scavenging activity and α-glucosidase inhibitory activity (13: IC50 46??M; 15: IC50 46??M). This is the first report identifying the DPPH free radical scavenging and α-glucosidase inhibitory activities of piperic acid amides and suggests that these amides may serve as lead compounds for the development of novel α-glucosidase inhibitors with antioxidant activity.
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http://libir.josai.ac.jp/il/user_contents/02/G0000284repository/pdf/JOS-cpb.c14-00874.pdf

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