Synthesis, structure and quantitative structure-activity relationships of σ receptor ligands, 1-[2-(3, 4-dimethoxyphenyl) ethyl]-4-(3-phenylpropyl) piperazines

K Fujimura, J Matsumoto, M Niwa, T Kobayashi…

Index: Fujimura, Ken-Ichi; Matsumoto, Junzo; Niwa, Masashi; Kobayashi, Tadayuki; Kawashima, Yoichi; In, Yasuko; Ishida, Toshimasa Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 8 p. 1675 - 1683

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Citation Number: 40

Abstract

A set of the title compounds having different substituents (R1, R2) on their phenyl groups was synthesized to find σ receptor binding affinity. Among the compounds, 2b (R1 R2 Cl) has the most potent σ1-binding activity, while 2a (R1 R2 H, SA4503) was most selective to σ1 over σ2 receptor. The crystal structures of 2a and 2b were shown, by X-ray crystallography, to be similar except for the one torsional angle of their propylene parts. ...