ACAT inhibitors derived from hetero-Diels-Alder cycloadducts of thioaldehydes

…, DL Burcham, SM Huang, JD Klaczkiewicz…

文献索引：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. Bioorganic and Medicinal Chemistry, 1996 , vol. 4, # 9 p. 1493 - 1513

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被引用次数: 17

摘要

Acyl-CoA: cholesterol acyltransferase (ACAT) is the enzyme largely responsible for intracellular cholesterol 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 ...