Potent Inhibitors of Acyl-CoA: Cholesterol Acyltransferase. Structure-Activity Relationships of Novel N-(4-Oxo-8-chromanyl) amides

…, T Takeyasu, T Mochizuki, K Taneda…

Index: Kataoka, Ken-ichiro; Shiota, Tatsuki; Takeyasu, Takumi; Mochizuki, Tsutomu; Taneda, Keiko; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 16 p. 3174 - 3186

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Citation Number: 14

Abstract

Introduction of a highly lipophilic alkoxy group at position 7 of the 4-chromanone moiety instead of methoxy group also resulted in potent activity. In this case, highest inhibitory activity was obtained by N-[7-(decyloxy)-4-oxochroman-8-yll-2, 2-dimethylpropanamide (65). The most potent compound, N-(7-methoxy-4-oxochroman-8-yl)-2, 2-dimethyldodecanamide (35, TEI-6522), showed significant ACAT inhibitory activity (rabbit small intestine IC50= 13 ...