title: New isoxazole derivatives designed as nicotinic acetylcholine receptor ligand candidates.
abstract: In this work we report the synthesis and evaluation of the analgesic properties of new isosteric heterocyclic derivatives, presenting the isoxazole nucleus, designed as nicotinic acetylcholine receptor ligand candidates, analogues to alkaloid epibatidine. Compound 2-(3-methyl-5-isoxazolyl)pyridine (3) presented the best analgesic profile of this series in hot plate test, which was partially prevented by pretreatment with nicotinic receptor antagonist mecamylamine.
authors.affiliation: Laboratório de Avaliação e Síntese de Substâncias Bioativas, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, PO Box 68006, 21944-970 Rio de Janeiro, RJ, Brazil.
authors.forename: Nilda M
authors.initials: NM
authors.lastname: Silva
authors.forename: Jorge L M
authors.initials: JL
authors.lastname: Tributino
authors.forename: Ana L P
authors.initials: AL
authors.lastname: Miranda
authors.forename: Eliezer J
authors.initials: EJ
authors.lastname: Barreiro
authors.forename: Carlos A M
authors.initials: CA
authors.lastname: Fraga
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D004353:Drug Evaluation, Preclinical; D005260:Female; D007555:Isoxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D008024:Ligands; D008297:Male; D051379:Mice; D015394:Molecular Structure; D018733:Nicotinic Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D011978:Receptors, Nicotinic / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D000700:Analgesics; D007555:Isoxazoles; D008024:Ligands; D018733:Nicotinic Antagonists; D011978:Receptors, Nicotinic