Synthesis and analgesic activities of some (4-substituted phenyl-1-piperazinyl)alkyl 2-aminobenzoates and 2-aminonicotinates.

doi:10.1021/JM00191A017

Paper

Synthesis and analgesic activities of some (4-substituted phenyl-1-piperazinyl)alkyl 2-aminobenzoates and 2-aminonicotinates.

Published May 1, 1979 · P. Manoury, A. Dumas, H. Najer

Journal of medicinal chemistry

Q1 SJR score

21

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0

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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.

Non-RCT

Animal Study

Study Snapshot

Antrafenine, a 4-substituted phenyl-1-piperazinyl alkyl 2-aminobenzoate, shows marked analgesic activity, long duration of action, and excellent tolerance in pharmacological and toxicological studies.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis and analgesic activities of some (4-substituted phenyl-1-piperazinyl)alkyl 2-aminobenzoates and 2-aminonicotinates.

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References

Citations

Anti-influenza virus activities and mechanism of antrafenine analogs.

Antrafenine analogs show good potency against influenza A strains, with potential for further development as anti-influenza agents.

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N,N'-Bisoxalamides Enhance the Catalytic Activity in Cu-Catalyzed Coupling of (Hetero)Aryl Bromides with Anilines and Secondary Amines.

N,N'-Bis(furan-2-ylmethyl)oxalamide (BFMO) enhances the catalytic activity in Cu-catalyzed N-arylation of anilines and cyclic secondary amines, enabling the coupling of various (hetero)aryl bro

Convenient Synthesis of Piperazine Substituted Quinolones

This study demonstrates a convenient method for synthesis of piperazine-substituted quinolones by direct condensation of ethyl [4-hydroxy-2-oxo-1-phenyl-1,2-dihydro-3-quinoline] carboxylate 2 with N1-