[Synthesis and analgesic activity of non-aryl analogues of 4-methoxycarbonyl fentanyl].
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.
Wen
S T
ST
Nanjing General Hospital of Nanjing Armed Forces.
Yang
Y L
YL
Shao
H Z
HZ
Zhang
K G
KG
Li
Y L
YL
Chen
J S
JS
D000701:Analgesics, Opioid / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D005260:Female; D005283:Fentanyl / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D017288:Pain Threshold / Q000187:drug effects; D013329:Structure-Activity Relationship
D000701:Analgesics, Opioid; C017114:carfentanil; D005283:Fentanyl