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

…, M Patel, Y Zhu, TR Stouch, D Bassolino-Klimas…

Index: Sulsky, Richard; Magnin, David R.; Huang, Yanting; Simpkins, Ligaya; Taunk, Prakash; Patel, Manorama; Zhu, Yeheng; Stouch, Terry R.; Bassolino-Klimas, Donna; Parker, Rex; Harrity, Thomas; Stoffel, Robert; Taylor, David S.; Lavoie, Thomas B.; Kish, Kevin; Jacobson, Bruce L.; Sheriff, Steven; Adam, Leonard P.; Ewing, William R.; Robl, Jeffrey A. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 12 p. 3511 - 3515

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Citation Number: 71

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.