Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: ureas bearing two heterocyclic head groups
โ Scribed by Richard G. Wilde; Jeffrey T. Billheimer
- Book ID
- 103982817
- Publisher
- Elsevier Science
- Year
- 1995
- Tongue
- English
- Weight
- 232 KB
- Volume
- 5
- Category
- Article
- ISSN
- 0960-894X
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โฆ Synopsis
A series of compounds bearing two heterocyclic substituents were prepared, and evaluated for inhibition of aeyl-CoA:cholesterol acyltransferase (ACAT). The heterocyclic groups were chosen for dual potency against hepatic and macrophage cell ACAT. Several examples of ACAT-balanced compounds were discovered, and the results of this study, including synthesis, are presented.
๐ SIMILAR VOLUMES
Acyl-CoA:cholesterol acyltransferase (E.C.2.3.1.26, ACAT) is a microsomial enzyme that catalyses the formation of cholesteryl esters by acylation of cholesterol with long chain fatty acylCoA [1]. ACAT plays important roles in cellular homeostasis and in the early stages of atherosclerosis. Therefor
A novel series of tetrazole-substituted ureas 2 were prepared from weakly nucleophilic amines using a new coupling method. The ureas were found to potently inhibit liver ACAT in vitro and lower total serum cholesterol in vivo. A comparison of urea 2b and the anti-atherosclerotic CI-976 in a long-ter