2. Academic Validation
  3. Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP)

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

Affiliation

  • 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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