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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
1992-10-26
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pubmed:abstractText |
Reaction of some picolines 5 with 1-chloro-2,4-dinitrobenzene (6) in acetone furnished methyl-substituted 2,4-dinitrophenylpyridinium chlorides 7. Further reaction with phenyl(pyridyl)carbonyl hydrazides 8 at room temperature furnished isolable 2,4-dinitroanilino derivatives 9, which were then refluxed in a water:dioxane mixture (1:4, v/v) to furnish the methyl-substituted phenyl(pyridyl)carbonyl iminopyridinium ylides 10. Reduction of the ylides with NaBH4 finally gave rise to the desired methyl-substituted phenyl(pyridyl)carbonylamino-1,2,3,6-tetrahydropyridines 11. The anti-inflammatory activities of 11a-11l were determined with the carrageenan-soaked sponge model of inflammation in Sprague-Dawley rats, and the analgesic effects of these derivatives were assessed by suppression of acetic acid-induced writhing in male Swiss albino mice. All compounds tested showed moderate to good anti-inflammatory and analgesic effects compared with indomethacin. Compound 11k was the most active analgesic, and 11h was the most effective anti-inflammatory agent among the methyl-substituted tetrahydropyridines.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0022-3549
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
81
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
463-6
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:1403681-Animals,
pubmed-meshheading:1403681-Anti-Inflammatory Agents, Non-Steroidal,
pubmed-meshheading:1403681-Drug Evaluation, Preclinical,
pubmed-meshheading:1403681-Male,
pubmed-meshheading:1403681-Mice,
pubmed-meshheading:1403681-Pyridines,
pubmed-meshheading:1403681-Pyridinium Compounds,
pubmed-meshheading:1403681-Rats
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pubmed:year |
1992
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pubmed:articleTitle |
Synthesis and pharmacological evaluation of some N-[pyridyl(phenyl)carbonylamino]methyl-1,2,3,6-tetrahydropyrid ines.
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pubmed:affiliation |
College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee 32307.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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