Stratford E S, Smith L M, Tomecko G W
J Pharm Sci. 1978 Jan;67(1):80-3. doi: 10.1002/jps.2600670120.
The synthesis and preliminary biological testing for in vitro cholesterol biosynthesis inhibitory activity of 2-indeneacetic acid, 2-methyl-1,2-dihydro-2-naphthoic acid, and their 5- and 7-chloro derivatives, respectively are described. These compounds were prepared as trans- and cis-analogs of the known antilipemic agent 3-methyl-4-phenyl-3-butenoic acid. Although both series of compounds showed cholesterol biosynthesis inhibitory properties, chloro substitution enhanced potency only in the cis-system. These findings are discussed in terms of a possible relationship between the cis-compounds and clofibrate-type antilipemic agents.
分别描述了2-茚乙酸、2-甲基-1,2-二氢-2-萘甲酸及其5-氯和7-氯衍生物的体外胆固醇生物合成抑制活性的合成及初步生物学测试。这些化合物被制备为已知抗血脂药3-甲基-4-苯基-3-丁烯酸的反式和顺式类似物。尽管这两个系列的化合物均显示出胆固醇生物合成抑制特性，但氯取代仅在顺式体系中增强了效力。根据顺式化合物与氯贝丁酯类抗血脂药之间可能的关系对这些发现进行了讨论。
