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Bioorg Med Chem Lett. 2007 Jun 15;17(12):3511-5. Epub 2006 Dec 21.

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

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  • 1Department of Metabolic Disease Chemistry, Bristol Myers-Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. sulskyr@bms.com


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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