4-苄氧基苯甲酸乙酯的降血脂类似物。

Hypolipidemic analogues of ethyl 4-benzyloxybenzoate.

作者信息

Baggaley K H, Fears R, Hindley R M, Morgan B, Murrell E, Thorne D E

出版信息

J Med Chem. 1977 Nov;20(11):1388-93. doi: 10.1021/jm00221a007.

Abstract

A series of compounds related to ethyl 4-benzyloxybenzoate was synthesized and evaluated for potential hypolipidemic activity in rats. Structure--activity relationships are discussed in terms of cholesterol-lowering activity together with effects on weight gain and liver lipids. A number of the compounds inhibited cholesterol and free fatty acid biosynthesis from [1-14C]acetate in rat liver slices in vitro. Ethyl 4-benzyloxybenzoate, ethyl-4-benzyloxybenzoic acid, ethyl 4-p-bromobenzyloxybenzoates, and 4-o-methoxybenzyloxyphenyl acetate exhibited the most favorable spectrum of activity.

摘要

合成了一系列与4-苄氧基苯甲酸乙酯相关的化合物，并在大鼠中评估其潜在的降血脂活性。从降低胆固醇活性以及对体重增加和肝脏脂质的影响方面讨论了构效关系。许多化合物在体外抑制大鼠肝切片中由[1-¹⁴C]乙酸合成胆固醇和游离脂肪酸。4-苄氧基苯甲酸乙酯、4-苄氧基苯甲酸、4-对溴苄氧基苯甲酸乙酯和4-邻甲氧基苄氧基苯基乙酸酯表现出最有利的活性谱。