Synthesis and activity of 2-methyl-3-aminopropiophenones as centrally acting muscle relaxants

…, G Izumi, S Kurashige, K Sakitama, M Ishikawa

Index: Shiozawa; Narita; Izumi; Kurashige; Sakitama; Ishikawa European Journal of Medicinal Chemistry, 1995 , vol. 30, # 1 p. 85 - 94

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Citation Number: 27

Abstract

Some novel 2-methyl-3-aminopropiophenones were synthesized and their centrally acting muscle relaxant activities were evaluated for an inhibitory effect on the flexor reflex in rats. The structure-activity relationships are discussed. In this series, 2-methyl-3-pyrrolidino-1-(4- trifluoromethylphenyl)-propan-1-one (28) showed significant centrally acting muscle relaxant activity. In addition, the activities of each enantiomer (28-(S) and (R) were studied along ...