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

Toshihiko Okada; Makoto Hiromura; Masato Otsuka; Shuichi Enomoto; Hiroyuki Miyachi

doi:10.1248/cpb.60.164

Notes

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

Toshihiko Okada, Makoto Hiromura, Masato Otsuka, Shuichi Enomoto, Hiroyuki Miyachi

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Keywords: fatty acid binding protein 4, BMS-309403, radioligand, labelled synthesis, C-14, adipocyte fatty acid binding protein

JOURNAL FREE ACCESS

2012 Volume 60 Issue 1 Pages 164-168

DOI https://doi.org/10.1248/cpb.60.164

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Abstract

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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