CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability

…, M Nguyen, S Kerwar, N Chu, D Soohoo, J Hao…

Index: Elzein, Elfatih; Ibrahim, Prabha; Koltun, Dmitry O.; Rehder, Ken; Shenk, Kevin D.; Marquart, Timothy A.; Jiang, Bob; Li, Xiaofen; Natero, Reina; Li, Yuan; Nguyen, Marie; Kerwar, Suresh; Chu, Nancy; Soohoo, Daniel; Hao, Jia; Maydanik, Victoria Y.; Lustig, David A.; Zeng, Dewan; Leung, Kwan; Zablocki, Jeff A. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 24 p. 6017 - 6021

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Citation Number: 23

Abstract

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= 380nM rat mitochondria) with favorable PK properties (F= 93%, t1/2= 13.6 h, dog).