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

Research output: Contribution to journalArticlepeer-review

4 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)164-168
Number of pages5
JournalChemical and Pharmaceutical Bulletin
Volume60
Issue number1
DOIs
Publication statusPublished - Jan 2012

Keywords

  • Adipocyte fatty acid binding protein
  • BMS-309403
  • C-14
  • Fatty acid binding protein 4
  • Labelled synthesis
  • Radioligand

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

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