Natsuka K, Nakamura H, Negoro T, Uno H, Nishimura H
J Med Chem. 1978 Dec;21(12):1265-9. doi: 10.1021/jm00210a017.
Forty-six 1-cycloalkyl-4-(1,2-diphenylethyl)piperazines were synthesized. The influence of substituents on phenyl groups of 1-cycloalkyl-4-(1,2-diphenylethyl)piperazines 4a-c on the analgesic activity was investigated in experimental animals. The most active compounds, 5a-c, in this series had a m-hydroxyl group on the 2-phenyl group of 4a-c, while morphine has a phenolic hydroxyl group para to th- aminoethyl moiety. Their activities were 23-56 and 23-38 times those of their original compounds 4a-c and morphine, respectively, tested by the D'Amour-Smith method after subcutaneous administration.
合成了46种1-环烷基-4-(1,2-二苯乙基)哌嗪。研究了1-环烷基-4-(1,2-二苯乙基)哌嗪4a-c的苯基上取代基对实验动物镇痛活性的影响。该系列中活性最高的化合物5a-c在4a-c的2-苯基上有一个间羟基，而吗啡在氨基乙基部分的对位有一个酚羟基。经皮下给药后，用D'Amour-Smith法测试，它们的活性分别是其原化合物4a-c和吗啡的23 - 56倍和23 - 38倍。
