| 摘要 |
PURPOSE:To provide an N-substituted amide derivative having excellent selective kappa-receptor agonistic activity and useful as a low-toxic central analgesic free from habituation. CONSTITUTION:The compound of formula I [R<1> and R<2> are lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl or together with N form a ring; R<3> is H or lower alkyl; Ar is aryl; A is single bond or lower alkylene; R<4> is halogen, lower alkyl, OH, lower alkoxy, lower alkylsulfonyl or (substituted)cycloalkyl or bicycloalkyl], e.g. (S)-2-cyclohexyl-N-methyl-N-[1-phenyl-2-(1pyrrolidinyl) ethyl]acetamide hydrochloride. The compound can be produced by reacting a carboxylic acid of formula II or its reactive derivative with a diamine of formula III. |
