transN-Methyl-N-[2-(1-pyrrolidinyl) cyclohexyl] cycloprop-2-ene-1-carboxamides: Novel lipophilic kappa opioid agonists

V Sabin, DC Horwell, AT McKnight, P Broqua

文献索引：Sabin; Horwell; McKnight; Broqua Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 3 p. 291 - 296

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被引用次数: 8

摘要

The synthesis and kappa opioid agonist activities of some lipophilic analogues of the kappa opioid agonist U-50488 incorporating motifs bearing two aromatic rings in place of the 3, 4- dichlorophenyl group are described. Trans 2, 3-diphenyl-N-methyl-N [2-(1-pyrrolidinyl) cyclohexyl]-2-cyclopropene-1-carboxamide, 7, is a potent kappa opioid agonist. A diphenylcyclopropene analogue of CI-977, trans 2, 3-diphenyl-N-methyl-N-[7-(1- ...