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ACAT inhibitors derived from hetero-Diels-Alder cycloadducts of thioaldehydes
Authors:RG Wilde  JT Billheimer  SJ Germain  EA Hausner  PC Meunier  DA Munzer  JK Stoltenborg  PJ Gillies  DL Burcham  SM Huang  JD Klaczkiewicz  SS Ko  RR Wexler
Affiliation:DuPont Merck Pharmaceutical Company, DuPont Experimental Station, Wilmington, DE 19880-0500, USA.
Abstract: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 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.
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