- CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability.
CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability.
Bioorganic & medicinal chemistry letters (2004-11-18)
Elfatih Elzein, Prabha Ibrahim, Dmitry O Koltun, Ken Rehder, Kevin D Shenk, Timothy A Marquart, Bob Jiang, Xiaofen Li, Reina Natero, Yuan Li, Marie Nguyen, Suresh Kerwar, Nancy Chu, Daniel Soohoo, Jia Hao, Victoria Y Maydanik, David A Lustig, Dewan Zeng, Kwan Leung, Jeff A Zablocki
PMID15546720
ZUSAMMENFASSUNG
New inhibitors of palmitoyl-CoA oxidation are based on the introduction of nitrogen heterocycles in the 'Western Portion' of the molecule. SAR studies led to the discovery of CVT-4325 (shown), a potent FOXi (IC50=380 nM rat mitochondria) with favorable PK properties (F=93%, t(1/2)=13.6h, dog).
MATERIALIEN