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

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 r...

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Published in:Bioorganic & medicinal chemistry letters 2006-07, Vol.16 (13), p.3504-3509
Main Authors: 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
Format: Article
Language:English
Subjects:
Biginelli condensation
Biological and medical sciences
Cell Line
FATP4 inhibitor
Fatty acid
Fatty Acid Transport Proteins - antagonists & inhibitors
General and cellular metabolism. Vitamins
Humans
Medical sciences
Molecular Structure
Pharmacology. Drug treatments
Pyrimidinones - chemical synthesis
Pyrimidinones - chemistry
Pyrimidinones - pharmacology
Stereoisomerism
Structure-Activity Relationship
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Summary: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. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.03.102