| Literature DB >> 19772346 |
Casey C Cosner1, John T Markiewicz, Pauline Bourbon, Christopher J Mariani, Olaf Wiest, Madalina Rujoi, Anton I Rosenbaum, Amy Y Huang, Frederick R Maxfield, Paul Helquist.
Abstract
A five-step synthesis of an array of N-aryl-3-alkylidenepyrrolinones, which are potential Niemann-Pick type C (NPC) disease therapeutics, is described. The synthetic route allows for the production of analogues, including photoaffinity and biotinylated derivatives. Compound 1a increased esterification by acyl-coenzyme A:cholesteryl acyltransferase in NPC1 mutant cells. It also decreased LDL uptake and increased cholesterol efflux in both NPC1-deficient and normal cells.Entities:
Mesh：
Substances：
Year: 2009 PMID： 19772346 PMCID： PMC2791921 DOI： 10.1021/jm900707n
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446