Literature DB >> 580207

[Studies on chemical structure and analgetic activity of phenyl substituted aminomethylcyclohexanoles (author's transl)].

K Flick, E Frankus, E Friderichs.   

Abstract

Phenyl substituted aminomethylcycloalkanole derivatives were synthetized and tested for analgetic activity. Substances with a high ratio between acute toxicity and analgetic efficacy were selected for further investigations. Structure-activity relationships of this group were evaluated and compared with those of morphine and morphine-like 4-phenylpiperidino derivatives. The basic structural requirement for the new compounds is a cycloalkane ring with a phenyl group and a dimethylaminomethyl residue in ortho-position. The analgetic activity is improved if the aromatic ring is substituted with an oxygen containing group in meta-position. In contrast to classical narcotic analgesics the analgetic efficacy is not lost in derivatives bearing a hydrogen substituent at the central carbon atom.

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Year:  1978        PMID: 580207

Source DB:  PubMed          Journal:  Arzneimittelforschung        ISSN: 0004-4172


  2 in total

1.  In vitro metabolism of the analgesic agent, tramadol-N-oxide, in mouse, rat, and human.

Authors:  W N Wu; L A McKown; E E Codd; R B Raffa
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2002 Jul-Sep       Impact factor: 2.441

2.  Investigation of racial variations in the metabolism of tramadol.

Authors:  D S Ogunleye
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2001 Jan-Jun       Impact factor: 2.569

  2 in total

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