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

Yoko Beniyama; Kenji Matsuno; Hiroyuki Miyachi

doi:10.1016/j.bmcl.2013.01.054

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

Yoko Beniyama, Kenji Matsuno, Hiroyuki Miyachi

Research output: Contribution to journal › Article › peer-review

18 Citations (Scopus)

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.

Original language	English
Pages (from-to)	1662-1666
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	23
Issue number	6
DOIs	https://doi.org/10.1016/j.bmcl.2013.01.054
Publication status	Published - Mar 15 2013
Externally published	Yes

Keywords

FABP3
Heart fatty acid binding protein
Pyrazole
Structural design

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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