Ono S, Yamafuji T, Chaki H, Morita H, Todo Y, Maekawa M, Kitamura K, Tai M, Narita H
Research Laboratories, Toyama Chemical Co., Ltd., Japan.
Chem Pharm Bull (Tokyo). 1995 Sep;43(9):1488-91. doi: 10.1248/cpb.43.1488.
A series of 2-(2-aminoethoxy)-1-phenylethanols having a variety of N- and phenyl-substitution patterns as well as 5- and 6-membered heteroaryl counterparts of our prototype compound 1 (2-(2-dimethylaminoethoxy)-1-phenylethanol) have been prepared and evaluated for antiamnestic and antihypoxic activities. Compound 3b, the 3-methylphenyl analogue of 1, proved to be significantly more potent than 1 in reversing electroconvulsive shock-induced amnesia as well as CO2-induced learning-impairment in mice. It exhibited low acute toxicity in mice and afforded a greater brain/serum concentration ratio than 1 after oral administration to rats.
我们制备了一系列具有多种N-和苯基取代模式的2-(2-氨基乙氧基)-1-苯基乙醇，以及原型化合物1（2-(2-二甲基氨基乙氧基)-1-苯基乙醇）的5-和6-元杂芳基类似物，并对其抗遗忘和抗缺氧活性进行了评估。化合物3b是1的3-甲基苯基类似物，在逆转电惊厥休克诱导的失忆以及小鼠二氧化碳诱导的学习障碍方面，其效力明显高于1。它在小鼠中表现出低急性毒性，在对大鼠口服给药后，其脑/血清浓度比高于1。
