4,5-Functionalized 6-phenyl-3(2 H)-pyridazinones: synthesis and evaluation of antinociceptive activity

A series of 2-substituted 4,5-functionalized 6-phenyl-3(2 H)-pyridazinones were synthesized and their antinociceptive activities were evaluated in the mouse abdominal constriction model. Single dose studies showed that compounds 11, 18a and 23 were more active than the reference drug, Emorfazone, in...

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Bibliographic Details
Published inEuropean journal of medicinal chemistry Vol. 31; no. 1; pp. 65 - 70
Main Authors Dal Piaz, V, Giovannoni, MP, Ciciani, G, Barlocco, D, Giardina, G, Petrone, G, Clarke, GD
Format Journal Article
LanguageEnglish
Published PARIS CEDEX 15 Elsevier Masson SAS 1996
Elsevier
Subjects
Analgesics
Biological and medical sciences
Chemistry, Medicinal
Emorfazone / pyridazinone /antinociceptive activity
Life Sciences & Biomedicine
Medical sciences
Neuropharmacology
Pharmacology & Pharmacy
Pharmacology. Drug treatments
Science & Technology
Emorfazone / pyridazinone /antinociceptive activity
AGENTS
antinociceptive activity
Emorfazone
pyridazinone
Vertebrata
Mammalia
Analgesic
Structure activity relation
Mouse
Animal
Rodentia
Pyridazine derivatives
Chemical synthesis
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Summary:A series of 2-substituted 4,5-functionalized 6-phenyl-3(2 H)-pyridazinones were synthesized and their antinociceptive activities were evaluated in the mouse abdominal constriction model. Single dose studies showed that compounds 11, 18a and 23 were more active than the reference drug, Emorfazone, in inhibiting the effects of the noxious chemical stimulus, p-phenylquinone. Subsequent dose—response studies revealed 18a to be almost seven-fold more potent than Emorfazone.
ISSN:0223-5234
1768-3254
DOI:10.1016/S0223-5234(96)80008-0