Synthesis and antidiabetic activity of β-acetamido ketones

Xingya Zhang,Ju-fang Yan,Li Fan,Gong-bao Wang,Dacheng Yang

Published 2011 in Acta Pharmaceutica Sinica B

ABSTRACT

Abstract 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.

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