作者:E F Llama、C Del Campo、M Capo
DOI:10.1111/j.2042-7158.1991.tb05456.x
日期:2011.4.12
The preparation of analogues of fentanyl with N-phenyl replaced with a heterocyclic aromatic ring, and with N-alkyl/arylalkyl N-acyl substituents is reported. Only those compounds carrying an N-phenylethyl substituent were active in the rat tail-withdrawal test. Fentanyl (1) is the prototype of the 4-anilido-piperidine class of opioid analgesics (Casy & Parfitt 1986). Several recent publications (Casy
报道了芬太尼的类似物的制备,其中芬太尼具有被杂环芳族环取代的N-苯基和具有N-烷基/芳基烷基的N-酰基取代基。在大鼠的拔尾试验中,只有那些带有N-苯乙基取代基的化合物才具有活性。芬太尼(1)是阿片类镇痛药的4-苯胺基-哌啶类的原型(Casy&Parfitt 1986)。关于该系列的一些最新出版物(Casy&Huckstep 1988; Bagley et al 1989)已经处理了芬太尼分子的杂环和芳族修饰。尽管大多数新型衍生物的抗伤害力都比吗啡大,但与芬太尼本身相比,它们的活性却降低了。要获取有关该系列的结构反应关系的更多信息,