Synthesis and antidiabetic activity of β-acetamido ketones

This paper reports the use of trifluoroacetic acid as a catalyst in the Dakin–West reaction for the synthesis of β-acetamido ketones. The method has several advantages such as requiring only mild conditions and a low concentration of catalyst. Screening of 19 β-acetamido ketones for antidiabetic act...

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Bibliographic Details
Main Authors: Xing-hua Zhang, Ju-fang Yan, Li Fan, Gong-bao Wang, Da-cheng Yang
Format: Article
Language:English
Published: Elsevier 2011-08-01
Series:Acta Pharmaceutica Sinica B
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S221138351100044X
Description
Summary:This paper reports the use of trifluoroacetic acid as a catalyst in the Dakin–West reaction for the synthesis of β-acetamido ketones. The method has several advantages such as requiring only mild conditions and a low concentration of catalyst. Screening of 19 β-acetamido ketones for antidiabetic activity in vitro showed that their activity as peroxisome proliferator-activated receptor (PPAR) agonists and as dipeptidyl peptidase 4 (DPP-IV) inhibitors was fairly weak.
ISSN:2211-3835
2211-3843