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Eur J Med Chem ; 37(2): 163-70, 2002 Feb.
Article in English | MEDLINE | ID: mdl-11858848

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.


Subject(s)
Analgesics/chemistry , Analgesics/pharmacology , Isoxazoles/chemistry , Isoxazoles/pharmacology , Nicotinic Antagonists/chemistry , Nicotinic Antagonists/pharmacology , Receptors, Nicotinic/metabolism , Analgesics/chemical synthesis , Analgesics/metabolism , Animals , Drug Evaluation, Preclinical , Female , Isoxazoles/chemical synthesis , Isoxazoles/metabolism , Ligands , Male , Mice , Molecular Structure , Nicotinic Antagonists/chemical synthesis , Nicotinic Antagonists/metabolism , Structure-Activity Relationship
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