Synthesis and antidiabetic activity of β-acetamido ketones

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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Veröffentlicht in:Acta pharmaceutica Sinica. B 2011-08, Vol.1 (2), p.100-105
Hauptverfasser: Zhang, Xing-hua, Yan, Ju-fang, Fan, Li, Wang, Gong-bao, Yang, Da-cheng
Format: Artikel
Sprache:eng
Schlagworte:
4-Chloroacetophenone
Dakin–West reaction
Diabetes mellitus
Trifluoroacetic acid
β-Acetamido ketone
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Zusammenfassung: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
DOI:10.1016/j.apsb.2011.06.006