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

. 2006 Jul 1;16(13):3504-9.

doi: 10.1016/j.bmcl.2006.03.102. Epub 2006 Apr 27.

Bing Guan, James Brown, Courtney Cullis, Stephen M Condon, Tracy J Jenkins, Stephane Peluso, Yingchun Ye, Ruth E Gimeno, Sandhya Punreddy, Ying Sun, Hui Wu, Brian Hubbard, Virendar Kaushik, Peter Tummino, Praveen Sanchetti, Dong Yu Sun, Tom Daniels, Effie Tozzo, Suresh K Balani, Prakash Raman

Affiliations

• PMID: 16644217
• DOI: 10.1016/j.bmcl.2006.03.102

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

Christopher Blackburn et al. Bioorg Med Chem Lett. 2006.

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 -NO(2) and CF(3)) of the 4-aryl group led to active compounds. In two cases racemates were resolved and the S enantiomers shown to have higher potencies.

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