Chemical and Pharmaceutical Bulletin p. 1488 - 1491 (1995)
Update date:2022-08-05
Topics:
Ono
Yamafuji
Chaki
Morita
Todo
Maekawa
Kitamura
Tai
Narita
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 I 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.
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