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PMID: 16644217 Published · ppublish English Journal Article

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

Bioorganic & medicinal chemistry letters ·Vol. 16 ·No. 13 ·2006-07-01 ·Pages 3504-9

Blackburn C, Guan B, Brown J, Cullis C, Condon SM, Jenkins TJ, Peluso S, Ye Y, Gimeno RE, Punreddy S, Sun Y, Wu H, Hubbard B, Kaushik V, Tummino P, Sanchetti P, Yu Sun D, Daniels T, Tozzo E, Balani SK, Raman P

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.

MeSH Terms
Cell Line Fatty Acid Transport Proteins/antagonists & inhibitors Humans Molecular Structure Pyrimidinones/chemical synthesis,chemistry,pharmacology Stereoisomerism Structure-Activity Relationship
Chemicals
Fatty Acid Transport Proteins Pyrimidinones SLC27A4 protein, human
Authors & Affiliations
21 authors, click to expand affiliations / ORCID
Blackburn Christopher
Medicinal Chemistry, Millennium Pharmaceuticals, Inc., 40 Landsdowne St., Cambridge, MA 02139, USA. [email protected]
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
Article Info
Journal
Bioorganic & medicinal chemistry letters
Abbr.
Bioorg Med Chem Lett
ISSN
0960-894X
DOI
10.1016/j.bmcl.2006.03.102
Email
[email protected]
Published
2006-07-01
Epub
2006-00-27
Pages
3504-9
Language
English
Region
England
NLM ID
9107377
Subset
IM
External Links
PubMed source DOI: 10.1016/j.bmcl.2006.03.102 View journal details
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