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Merck
CN
  • 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).

Bioorganic & medicinal chemistry letters (2007-05-16)
Richard Sulsky, 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
摘要

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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