Synthesis and Analgesic Effect of N-Substituted 5-Arylidene-6-methyl-3-(4H)-pyridazinones

Two methods of N-substitution were applied to 5-arylidene-6-methyl-3-(4H)-pyridazinones. The resulting derivatives were tested in order to determine the area of pharmacological activity. Most compounds exhibited a dose-dependent analgesic activity. Introduction of a benzoyl substituent in the 2-posi...

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Bibliographic Details
Published inChemical & pharmaceutical bulletin Vol. 36; no. 4; pp. 1558 - 1561
Main Authors RUBAT, CATHERINE, COUDERT, PASCAL, COUQUELET, JACQUES, BASTIDE, PIERRE, BASTIDE, JEANINE
Format Journal Article
LanguageEnglish
Published Tokyo The Pharmaceutical Society of Japan 1988
Maruzen
Japan Science and Technology Agency
Subjects
Analgesics - chemical synthesis
Animals
anti-inflammatory activity
Chemical Phenomena
Chemistry
Exact sciences and technology
Heterocyclic compounds
Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings
Male
Mice
Organic chemistry
Preparations and properties
Pyridazines - chemical synthesis
Pyridazines - pharmacology
Organic hydrazide
Analgesic
Hydrochlorides
Nitrogen heterocycle
Six membered ring
Acyl halide
Halocarbon
Biological activity
Formaldehyde
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Summary:Two methods of N-substitution were applied to 5-arylidene-6-methyl-3-(4H)-pyridazinones. The resulting derivatives were tested in order to determine the area of pharmacological activity. Most compounds exhibited a dose-dependent analgesic activity. Introduction of a benzoyl substituent in the 2-position of the pyridazinone ring 2j induced the most potent activity.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.36.1558