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

Y Beniyama, K Matsuno, H Miyachi

Index: Beniyama, Yoko; Matsuno, Kenji; Miyachi, Hiroyuki Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 6 p. 1662 - 1666

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Citation Number: 5

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 ...