N-substituted aminohydroxypyridines as potential non-opioid analgesic agents Original Research Article

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.