ATP-citrate lyase as a target for hypolipidemic intervention. Design and synthesis of 2-substituted butanedioic acids as novel, potent inhibitors of the enzyme

…, A Shaw, D McNair, R Novelli, CE Novelli…

文献索引：Gribble, Andrew D.; Dolle, Roland E.; Shaw, Antony; McNair, David; Novelli, Riccardo; Novelli, Christine E.; Slingsby, Brian P.; Shah, Virendra P.; Tew, David; Saxty, Barbara A.; Allen, Mark; Groot, Pieter H.; Pearce, Nigel; Yates, John Journal of Medicinal Chemistry, 1996 , vol. 39, # 18 p. 3569 - 3584

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被引用次数: 25

摘要

ATP-citrate lyase is the primary enzyme responsible for the synthesis of cytosolic acetyl-CoA in many tissues. Inhibitors of the enzyme represent a potentially novel class of hypolipidemic agent, which are anticipated to have combined hypocholesterolemic and hypotriglyceridemic properties. A series of 2-substituted butanedioic acids have been designed and synthesized as inhibitors of the enzyme. The best compounds, 58, 68, 71, ...