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N-substituted aminohydroxypyridines as potential non-opioid analgesic agents. 1995
M C Viaud, and
P Jamoneau, and
J G Bizot-Espiard, and
B Pfeiffer, and
P Renard, and
D H Caignard, and
G Adam, and
G Guillaumet
Université d'Orléans Laboratoire de Chimie Bioorganique et Analytique (L.C.B.A.), URA CNRS n.499, Orléans, France.
A series of new N-substituted aminohydroxypyridines have been synthesized, pharmacologically evaluated and compared with their N-substituted oxazolopyridone analogs. The compound with the maximal combination of safety and analgesic efficacy was 3-[2-[4-(4-fluorophenyl)-1-piperazinyl]ethyl]amino-2-hydroxypyridine (compound 10a), with ED50 values 0.4 mg kg-1 po (mouse: phenylquinone writhing test) and 0.5 mg kg-1 po (rat: acetic acid writhing test). Compound 10a possesses a potent non-opioid antinociceptive activity with moderate anti-inflammatory properties.
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