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Citation: TANG Xuemei, FAN Li, ZHAO Qin, YANG Dacheng. Synthesis and Bioactivities of β-Amino Ketones Containing Sulfadiazine Moiety[J]. Chinese Journal of Applied Chemistry, ;2015, 32(11): 1231-1239. doi: 10.11944/j.issn.1000-0518.2015.11.150070 shu

Synthesis and Bioactivities of β-Amino Ketones Containing Sulfadiazine Moiety

TANG Xuemei ^a ,
FAN Li ^b ,
ZHAO Qin ^b ,
YANG Dacheng ^b,,

1.
a School of Life Science, Southwest University, Chongqing 400715, China;
2.
b School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China

Corresponding author: YANG Dacheng,
Received Date: 20 February 2015
Available Online: 17 June 2015
Fund Project: 中央高校基本业务费专项资金(XDJK2015C128) (XDJK2015C128)重庆市自然科学基金(2005BB5095)资助 (2005BB5095)

Sixteen new β-amino ketones containing sulfadiazine moiety have been directly synthesized through atom-economic Mannich reaction of sulfadiazine with 1-acetonaphthone and some aromatic aldehydes. The chemical structures of these obtained compounds were identified by ¹H NMR, ¹³C NMR,and HRMS. The biological assay results show that all obtained compounds in the concentration range of 17.04~19.69 nmol/L possess very weak α-glucosidase inhibitory activities, while some compounds can activate peroxisome proliferator-activated receptor response element(PPRE) moderately,of which one exhibits the strongest activity(52%).
- diabetes mellitus,
- peroxisome proliferator-activated receptor response element(PPRE),
- α-glucosidase,
- Mannich reaction,
- β-amino ketones,
- sulfadiazine
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