Synthesis of BMS-309403-Related Compounds, Including 〔¹⁴C〕BMS-309403, a Radioligand for Adipocyte Fatty Acid Binding Protein

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  • Okada Toshihiko
    Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University
  • Hiromura Makoto
    Laboratory of Multiple Molecular Imaging Research Center for Molecular Imaging Science, RIKEN Kobe Institute
  • Otsuka Masato
    Department of Genomics and Proteomics, Advanced Science Research Center, Okayama University
  • Enomoto Shuichi
    Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University Laboratory of Multiple Molecular Imaging Research Center for Molecular Imaging Science, RIKEN Kobe Institute
  • Miyachi Hiroyuki
    Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University

書誌事項

タイトル別名
  • Synthesis of BMS-309403-Related Compounds, Including [14C]BMS-309403, a Radioligand for Adipocyte Fatty Acid Binding Protein
  • ChemInform Abstract: Synthesis of BMS‐309403‐Related Compounds, Including [<sup>14</sup>C]BMS‐309403 (I), a Radioligand for Adipocyte Fatty Acid Binding Protein.

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説明

Adipocyte fatty acid binding protein (A-FABP; FABP4), which is predominantly expressed in macrophages and adipose tissue, regulates fatty acid storage and lipolysis, and is also an important mediator of inflammation. Here, we report a synthesis of 14C-labeled 2-[2′-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)biphenyl-3-yloxy]acetic acid (BMS309403), a potent and selective small-molecular FABP4 inhibitor, as a chemical tool for investigating the roles of FABP4 in inflammatory and metabolic disorders. The structure–activity relationship of several BMS derivatives for inhibition of FABP4 is also reported.

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