Synthesis of BMS-309403-Related Compounds, Including [14C]BMS-309403, a Radioligand for Adipocyte Fatty Acid Binding Protein
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概要
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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 sup14/supC-labeled 2-[2′-(5-ethyl-3,4-diphenyl-1iH/i-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.
- 公益社団法人 日本薬学会の論文
著者
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Otsuka Masato
Department Of Biochemistry Faculty Of Pharmaceutical Sciences Okayama University
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Hiruma Makoto
Department Of Analytical And Bioinorganic Chemistry Kyoto Pharmaceutical University
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Okada Toshihiko
Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University
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Miyachi Hiroyuki
Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University
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Hiromura Makoto
Laboratory of Multiple Molecular Imaging Research Center for Molecular Imaging Science, RIKEN Kobe Institute
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Enomoto Shuichi
Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University
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Otsuka Masato
Department of Genomics and Proteomics, Advanced Science Research Center, Okayama University
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