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New isoxazole derivatives designed as nicotinic acetylcholine receptor ligand candidates
Nilda M Silva1, Jorge L M Tributino, Ana L P Miranda
1Laboratório 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.
European Journal of Medicinal Chemistry
|February 23, 2002
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.