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 eelctroconvulsive 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.
Gilman; Fullhart, Journal of the American Chemical Society, 1949, vol. 71, p. 1478,1480
作者:Gilman、Fullhart
DOI:——
日期:——
Local Anesthetics III
作者:Seymour L. Shapiro、Harold Solo Way、Harris J. Shapiro、Louis Freedman
DOI:10.1002/jps.2600500913
日期:1961.9
Abstract A series of “procaine analogs” (I) was prepared by reaction of dialkylaminoalkoxyphenylethanols with aromatic acid chlorides. Upon evaluation as anesthetics, selected compounds showed considerably more activity than procaine.