Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP)

  • Bioorg Med Chem Lett. 2007 Jun 15;17(12):3511-5. doi: 10.1016/j.bmcl.2006.12.044.
Richard Sulsky  1 ,  David R Magnin ,  Yanting Huang ,  Ligaya Simpkins ,  Prakash Taunk ,  Manorama Patel ,  Yeheng Zhu ,  Terry R Stouch ,  Donna Bassolino-Klimas ,  Rex Parker ,  Thomas Harrity ,  Robert Stoffel ,  David S Taylor ,  Thomas B Lavoie ,  Kevin Kish ,  Bruce L Jacobson ,  Steven Sheriff ,  Leonard P Adam ,  William R Ewing ,  Jeffrey A Robl
Affiliations
  • 1. Department of Metabolic Disease Chemistry, Bristol Myers-Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. [email protected]
PMID: 17502136 DOI: 10.1016/j.bmcl.2006.12.044
Abstract

Herein we report the first disclosure of biphenyl azoles that are nanomolar Binders of adipocyte fatty acid binding protein (aFABP or aP2) with up to thousand-fold selectivity against muscle fatty acid binding protein and epidermal fatty acid binding protein. In addition a new radio-ligand to determine binding against the three fatty acid binding proteins was also synthesized.

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