Synthesis and κ binding affinity of 1-(pyrrolidin-1-ylmethyl)-2-(N-methyl)-4-[(3, 4-dichloro) phenyl]-1, 2, 3, 4 tetrahydroisoquinolin-3 (2H)-ones

GA Pinna, E Gavini, G Cignarella, S Scolastico…

文献索引：Pinna, G. A.; Gavini, E.; Cignarella, G.; Scolastico, S.; Fadda, P. European Journal of Medicinal Chemistry, 1995 , vol. 30, # 6 p. 515 - 520

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被引用次数: 2

摘要

Diastereomeric forms of l-(pyrrolidin-1-ylmethyl)-2-(N-methyl)-4-[(3, 4-dichloro) phenyl]-1, 2, 3, 4-tetrahydroisoquinol in-3 (2H)-ones 3a and its chloro analog 3c were synthesized. Compounds 3a, c are related to the κ-selective opiate ICI 199441 1 by linking the benzylic CH2 to the ortho position of the phenyl in 1. Compared with morphine, these compounds had lost in κ and κ affinities; only cis-3a showed a modest κ affinity. 1-Pyrrolidin-1-ylmethyl ...