183988-01-4Relevant academic research and scientific papers
ACAT inhibitors derived from hetero-Diels-Alder cycloadducts of thioaldehydes
Wilde, Richard G.,Billheimer, Jeffrey T.,Germain, Sandie J.,Hausner, Elizabeth A.,Meunier, Paul C.,Munzer, Deborah A.,Stoltenborg, Janet K.,Gillies, Peter J.,Burcham, Deborah L.,Huang, Shiew-Mai,Klaczkiewicz, John D.,Ko, Soo S.,Wexler, Ruth R.
, p. 1493 - 1513 (2007/10/03)
Acyl-CoA:cholesterol acyltransferase (ACAT) is the enzyme largely responsible for intracellular cholesteror esterification. A systemic inhibitor of ACAT is believed to be able to slow or even reverse the atherosclerotic process. Towards that goal, a series of cyclic sulfides, derived from the hetero-Diels-Alder reaction of thioaldehydes with 1,3-dienes, and bearing carboxamide substituents, were prepared and evaluated for in vitro (in several tissues and species) and ex vivo ACAT inhibition. Minor changes in subsequent structure were found to have a significant effect in optimization of the biological activity of this series of compounds.
