潜在的抗动脉粥样硬化剂。2. 西他本的（芳烷基氨基）和（烷基氨基）苯甲酸类似物。
Potential antiatherosclerotic agents. 2. (Aralkylamino)- and (alkylamino) benzoic acid analogues of cetaben.
作者信息
Albright J D, DeVries V G, Largis E E, Miner T G, Reich M F, Schaffer S A, Shepherd R G, Upeslacis J
出版信息
J Med Chem. 1983 Oct;26(10):1378-93. doi: 10.1021/jm00364a009.
The syntheses of a series of (aralkylamino)- and (alkylamino)benzoic acids, as well as the corresponding esters and sodium salts, are described. The compounds were evaluated in vivo in rats for serum sterol and triglyceride lowering activity and in vitro for activity in inhibiting the principle cholesterol-esterifying enzyme of the arterial wall, fatty acyl-CoA:cholesterol acyltransferase (ACAT). Based on a combination of these two activities, cataben sodium (150) was selected for development as a hypolipidemic and potential antiatherosclerotic agent.
本文描述了一系列（芳烷基氨基）苯甲酸和（烷基氨基）苯甲酸及其相应酯类和钠盐的合成方法。对这些化合物进行了大鼠体内血清固醇和甘油三酯降低活性评估，以及体外抑制动脉壁主要胆固醇酯化酶——脂肪酰辅酶A：胆固醇酰基转移酶（ACAT）活性的评估。基于这两种活性的综合表现，选择卡他苯钠（150）作为降血脂和潜在抗动脉粥样硬化药物进行开发。
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