Synthesis and Biological Evaluation of 3-Methyl-5-phenylthieno[2,3-<i>d</i>]pyrimidine-2,4(1<i>H</i>,3<i>H</i>)-dione Derivatives for the Treatment of Diet-Induced Obesity

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  • Sang Yun
    Chemistry College, Sichuan University
  • Pei Heyin
    State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University
  • Ma Liang
    State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University
  • Huang Li
    State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University
  • Xie Caifeng
    State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University
  • Chen Jinying
    State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University
  • Liang Xiaolin
    State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University
  • Ran Yan
    State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University
  • Wang Guangcheng
    State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University
  • Yang Zhuang
    Chemistry College, Sichuan University
  • Cao Dong
    State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University
  • He Lin
    State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University
  • Wu Yuzhe
    State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University
  • He Linhong
    State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University
  • Zhu Jun
    State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University
  • Lan Jingbo
    Chemistry College, Sichuan University
  • Chen Lijuan
    State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University

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  • Synthesis and Biological Evaluation of 3-Methyl-5-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione Derivatives for the Treatment of Diet-Induced Obesity

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Abstract

Triglycerides are the main part of fats and half of the lipids in hepatocytes, and play an important role in metabolism as energy sources and transporters of dietary fat. In this study, 33 derivatives based on 3-methyl-5-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione were synthesized and evaluated for their lipid-lowering activity. Among them, compound 1i was found to exhibit potent triglyceride-lowering potency in 3T3-L1 adipocytes which was comparable to that of the adenosine monophosphate-activated protein kinase (AMPK) agonist Acadesine (AIACR). Furthermore, oral administration of 1i at a dose of 50 mg kg−1 d−1 for 5 weeks could reduce the mean body weight and liver weight by 12.02% and 32.00%, respectively, and regulated serum levels of triglycerides in diet-induced obese mice. The results indicate that compound 1i is a potential small-molecule for the treatment of diet-induced obesity and related diseases.

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