Wen S T, Yang Y L, Shao H Z, Zhang K G, Li Y L, Chen J S
Nanjing General Hospital of Nanjing Armed Forces.
Yao Xue Xue Bao. 1993;28(3):181-7.
In this paper, the synthesis and analgesic activities of some derivatives of 4-methoxycarbonyl fentanyl are reported, in which the 4-N-phenyl group or both the 4-N-phenyl group and the 1-beta-phenyl group were replaced by some nonaromatic groups. In the last case, some compounds showed very strong analgesic activity. For example, the analgesic activities of compounds 4 and 6 were shown to be 695 and 818 times more potent than that of morphine respectively. The structure-analgesic activity relationships were discussed.
本文报道了4-甲氧羰基芬太尼的一些衍生物的合成及其镇痛活性，其中4-N-苯基或4-N-苯基和1-β-苯基均被一些非芳香族基团取代。在后一种情况下，一些化合物表现出非常强的镇痛活性。例如，化合物4和6的镇痛活性分别比吗啡强695倍和818倍。文中还讨论了结构与镇痛活性的关系。
