Acyl-CoA: cholesterol O-acyl transferase (ACAT) inhibitors. 1. 2-(Alkylthio)-4, 5-diphenyl-1H-imidazoles as potent inhibitors of ACAT

NV Harris, AW Bridge, RC Bush…

Index: Harris, Neil V.; Smith, Christopher; Asthon, Michael J.; Bridge, Andrew W.; Bush, Raymond C.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 23 p. 4384 - 4392

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Citation Number: 40

Abstract

A potent, bioavailable ACAT inhibitor may have beneficial effects in the treatment of atherosclerosis by (i) reducing the absorption of dietary cholesterol,(ii) reducing the secretion of very low density lipoproteins into plasma from the liver, and (iii) preventing the transformation of arterial macrophages into foam cells. We have found that a mevalonate derivative 2, which contains a 4, 5-diphenyl-lH-imidazol-2-y1 moiety, inhibits rat hepatic ...