ACAT inhibitors derived from hetero-Diels-Alder cycloadducts of thioaldehydes
作者： Richard G. Wilde , Jeffrey T. Billheimer , Sandie J. Germain , Elizabeth A. Hausner , Paul C. Meunier
DOI: 10.1016/0968-0896(96)00143-5
关键词:
摘要: Acyl-CoA:cholesterol acyltransferase (ACAT) is the enzyme largely responsible for intracellular cholesterol esterification. A systemic inhibitor of ACAT believed to be able slow or even reverse atherosclerotic process. Towards that goal, a series cyclic sulfides, derived from hetero-Diels-Alder reaction thioaldehydes with 1,3-dienes, and bearing carboxamide substituents, were prepared evaluated in vitro (in several tissues species) ex vivo inhibition. Minor changes subsequent structure found have significant effect optimization biological activity this compounds.
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