Synthesis and analgesic activity of some spiro[dibenz[b,f]oxepin-10,4'-piperidine] derivatives
- 1 July 1979
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 22 (7) , 834-839
- https://doi.org/10.1021/jm00193a016
Abstract
A series of 10,11-dihydro-11-oxospiro[dibenz[b,f]oxepin-10,4''-piperidine] derivatives was synthesized and evaluated for analgesic activity in the phenylquinone writhing assay (PQW) and the tail-flick test in mice. Preliminary structure-activity correlations indicate that optimum activity is associated with a short-chain (R .ltoreq. C2) N substituent and a nuclear fluorine function as exemplified by 9b. This compound when administered orally was equipotent to morphine in protecting against mouse writhing. The observation that the PQW activity of 9b remained relatively unchanged after naloxone challenge seems to favor a nonnarcotic profile.This publication has 1 reference indexed in Scilit:
- A Method for Evaluating both Non-Narcotic and Narcotic AnalgesicsExperimental Biology and Medicine, 1957