Kawamatsu Y, Asakawa H, Saraie T, Imamiya E, Nishikawa K, Hamuro Y
Arzneimittelforschung. 1980;30(4):585-9. doi: 10.1002/chin.198031181.
alpha-Substituted-beta-arylpropionic acid derivatives were prepared and examined for hypolipidemic activity. The structure-activity relationship study showed that a chloro substituent at the alpha-position and an aryloxy or aralkyloxy substituent on the beta-aryl moiety was necessary for possession of substantial activity. In addition, some of these compounds showed hypolipidemic and hypoglycemic effects on diabetic mice. Among the 71 compounds prepared, ethyl 2-chloro-3-[4-(4-chlorobenzyloxy)phenyl]propionate (12) and ethyl 2-chloro-3-[4-(1-phenylethyloxy)phenyl]propionate (24) were the best with respect to activity and toxicity.
制备了α-取代-β-芳基丙酸衍生物并检测其降血脂活性。构效关系研究表明，α位的氯取代基和β-芳基部分上的芳氧基或芳烷氧基取代基是具有显著活性所必需的。此外，其中一些化合物对糖尿病小鼠表现出降血脂和降血糖作用。在所制备的71种化合物中，2-氯-3-[4-(4-氯苄氧基)苯基]丙酸乙酯(12)和2-氯-3-[4-(1-苯乙氧基)苯基]丙酸乙酯(24)在活性和毒性方面表现最佳。
