## Abstract For Abstract see ChemInform Abstract in Full Text.
Pyridazine derivatives as novel acyl-coa:cholesterol acyltransferase (acat) inhibitors
โ Scribed by Arianna Gelain
- Book ID
- 102343911
- Publisher
- Journal of Heterocyclic Chemistry
- Year
- 2005
- Tongue
- English
- Weight
- 96 KB
- Volume
- 42
- Category
- Article
- ISSN
- 0022-152X
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โฆ Synopsis
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. Therefore, ACAT inhibitors have been identified as useful agents in the treatment of hypercholesterolemia, atherosclerosis and coronary diseases [2]. In addition, recently their application has been proposed for Alzheimer's disease [3].
๐ SIMILAR VOLUMES
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 disc