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Bioorg Med Chem Lett. 2013 Mar 15;23(6):1662-6. doi: 10.1016/j.bmcl.2013.01.054. Epub 2013 Jan 26.

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

Author information

1
Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University 1-1-1, Tsushima-Naka, Kita-ku, Okayama 700-8530, Japan.

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.

PMID:
23395658
DOI:
10.1016/j.bmcl.2013.01.054
[Indexed for MEDLINE]

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