Synthesis and structure-activity relationships of 1-substituted 4-(1, 2-diphenylethyl) piperazine derivatives having narcotic agonist and antagonist activity

K Natsuka, H Nakamura, Y Nishikawa…

Index: Natsuka; Nakamura; Nishikawa; Negoro; Uno; Nishimura Journal of Medicinal Chemistry, 1987 , vol. 30, # 10 p. 1779 - 1787

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Citation Number: 12

Abstract

Racemates and enantiomers of 1-substituted 4-[2-(3-hydroxyphenyl)-l-phenylethyl] piperazine derivatives (3-18) were synthesized, and their analgesic and other pharmacological activities and structure-activity relationships were investigated. The S-(+) enantiomers of 2a, 5, 7, 9, 10, and 15-18 had a stronger analgesic activity than their R-(-) enantiomers; analgesic activity of the strongest one [(S)-(+)-lO] was 105 times as potent as ...