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本文报道了某些к-型阿片受体激动剂U-50488结构类似物的合成。在小白鼠热板试验和扭体试验的结果表明,反式环己二胺结构中2位氨基为五元环吡咯啉基时对к-活性有重要作用。以六元环氯基(哌啶基、哌嗪基,吗啉基)取代2位五元环氯基导致,к-活性降低。另外,也探讨了1位芳酰氨基结构改变对к-活性的影响。
This paper reports the synthesis of certain analogues of the к-opioid receptor agonist U-50488. The results of the hot plate test and the writhing test in mice showed that the 2-amino group in the trans-cyclohexanediamine structure plays an important role in the к-activity when it is a 5-membered ring pyrrolinyl group. Substitution of a six-membered ring chloro group (piperidinyl, piperazinyl, morpholinyl) for a five-membered ring with two-position causes a decrease in к-activity. In addition, the effect of the structural change of the 1-arylamino group on the к-activity was also investigated.