Identification and characterization of 4-aryl-3, 4-dihydropyrimidin-2 (1H)-ones as inhibitors of the fatty acid transporter FATP4

…, J Brown, C Cullis, SM Condon, TJ Jenkins…

Index: Blackburn, Christopher; Guan, Bing; Brown, James; Cullis, Courtney; Condon, Stephen M.; Jenkins, Tracy J.; Peluso, Stephane; Ye, Yingchun; Gimeno, Ruth E.; Punreddy, Sandhya; Sun, Ying; Wu, Hui; Hubbard, Brian; Kaushik, Virendar; Tummino, Peter; Sanchetti, Praveen; Yu Sun, Dong; Daniels, Tom; Tozzo, Effie; Balani, Suresh K.; Raman, Prakash Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 13 p. 3504 - 3509

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Citation Number: 58

Abstract

Several potent, cell permeable 4-aryl-dihydropyrimidinones have been identified as inhibitors of FATP4. Lipophilic ester substituents at the 5-position and substitution at the para- position (optimal groups being–NO2 and CF3) of the 4-aryl group led to active compounds. In two cases racemates were resolved and the S enantiomers shown to have higher potencies.