1. Synthesis and analgesic activities of some (4-substituted phenyl-1-piperazinyl)alkyl 2-aminobenzoates and 2-aminonicotinates.
- Author
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Manoury PM, Dumas AP, Najer H, Branceni D, Prouteau M, and Lefevre-Borg FM
- Subjects
- Acetates antagonists & inhibitors, Aminobenzoates pharmacology, Aminobenzoates toxicity, Animals, Anti-Inflammatory Agents chemical synthesis, Carrageenan, Edema physiopathology, Lethal Dose 50, Male, Mice, Nicotinic Acids pharmacology, Nicotinic Acids toxicity, Rats, Reaction Time drug effects, Structure-Activity Relationship, Aminobenzoates chemical synthesis, Analgesics chemical synthesis, Nicotinic Acids chemical synthesis
- Abstract
A series of (4-substituted phenyl-1-piperazinyl)alkyl 2-aminobenzoates and 2-aminonicotinates has been prepared and screened for analgesic and antiinflammatory properties in mice and rats. The tabulated results reveal several 2-(4-substituted phenyl-1-piperazinyl)ethyl 2-(7- or 8-substituted 4-quinolinylamino)benzoates to be six to nine times more potent analgesics than the reference compounds (glafenine and aminopyrine) and to possess minor antinflammatory activity. Compound 45, 2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl 2-[[7-(trifluoromethyl)-4-quinolinyl]amino]benzoate (antrafenine), showed marked analgesic activity, long duration of action, and excellent tolerance in pharmacological and toxicological studies, as well as in clinical trials.
- Published
- 1979
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