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N-substituted aminohydroxypyridines as potential non-opioid analgesic agents
M C Viaud1, P Jamoneau, J G Bizot-Espiard
1Université d'Orléans Laboratoire de Chimie Bioorganique et Analytique (L.C.B.A.), URA CNRS n.499, Orléans, France.
Bioorganic & Medicinal Chemistry
|July 1, 1995
Abstract:
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.