Structure-guided design, synthesis and in vitro evaluation of a series of pyrazole-based fatty acid binding protein (FABP) 3 ligands

  • Bioorg Med Chem Lett. 2013 Mar 15;23(6):1662-6. doi: 10.1016/j.bmcl.2013.01.054.
Yoko Beniyama  1 ,  Kenji Matsuno ,  Hiroyuki Miyachi
Affiliations
  • 1. Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University 1-1-1, Tsushima-Naka, Kita-ku, Okayama 700-8530, Japan.
PMID: 23395658 DOI: 10.1016/j.bmcl.2013.01.054
Abstract

We designed a series of pyrazole-based carboxylic acids as candidate ligands of heart fatty acid binding protein (H-FABP, or FABP3), based on a comparison of the X-ray crystallographic structures of adipocyte fatty acid binding protein (FABP4)-selective inhibitor (BMS309403) complex and FABP3-elaidic acid complex. Some of the synthesized compounds exhibited dual FABP3/4 ligand activity, and some exhibited selectivity for FABP3.

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