title: N-substituted aminohydroxypyridines as potential non-opioid analgesic agents.
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.
authors.affiliation: Université d'Orléans Laboratoire de Chimie Bioorganique et Analytique (L.C.B.A.), URA CNRS n.499, Orléans, France.
authors.forename: M C
authors.initials: MC
authors.lastname: Viaud
authors.forename: P
authors.initials: P
authors.lastname: Jamoneau
authors.forename: J G
authors.initials: JG
authors.lastname: Bizot-Espiard
authors.forename: B
authors.initials: B
authors.lastname: Pfeiffer
authors.forename: P
authors.initials: P
authors.lastname: Renard
authors.forename: D H
authors.initials: DH
authors.lastname: Caignard
authors.forename: G
authors.initials: G
authors.lastname: Adam
authors.forename: G
authors.initials: G
authors.lastname: Guillaumet
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000494:pharmacology*; D005260:Female; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D011725:Pyridines; C014047:hydroxypyridines