4-Anilidopiperidine Analgesics I: Synthesis and Analgesic Activity of Certain Ring-Methylated 1-Substituted 4-Propananilidopiperidines

Autor: Danny B. Hale, Thomas N. Riley, Marvin C. Wilson
Rok vydání: 1973
Předmět:
Zdroj: Journal of Pharmaceutical Sciences. 62:983-986
ISSN: 0022-3549
DOI: 10.1002/jps.2600620627
Popis: In view of the potency-enhancing effect of methyl substitution of the piperidine ring of the 4-phenylpiperidine analgesics and (he alkylene chain of the acyclic basic anilide analgesics, the 1-methyl, 1-benzyl, and 1-phenylethyl derivatives of 2-methyl-, 3-methyl-, and 2,5-dimethyl-4-propananilidopiperidine were prepared. The analgesic activity of these compounds indicates that 3- methylation has the greatest effect in enhancing analgesjc potency whereas 2-methyl and 2,5-dimethyl substitution is detrimental to analgesic activity.
Databáze: OpenAIRE