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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
9
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pubmed:dateCreated |
1995-6-7
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pubmed:abstractText |
Modification of some 8-benzylidene-5,6,7,8-tetrahydroquinolines, which have good antiulcer activity, led to three distinct classes of compounds with good in vivo antiinflammatory activity. Initial efforts led to a series of alkenes derived from 5,6,7,8-tetrahydroquinolines substituted at the 8-position. A second approach concentrated on replacing the CH linkage of these 8-benzylidene-substituted compounds with other spacer groups and increasing the size of the cycloalkyl ring from a six- to seven-membered ring, which provided 6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridine analogues. Finally, the substituent was switched from the cycloalkyl ring to the 2-position of the pyridine ring. Variation of the 2-substituent was also examined. Optimal antiinflammatory activity after oral administration was found in both the rat carrageenan paw edema and rat developing adjuvant arthritis models with 2-substituted 6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridines, and of particular interest was 27 (WY-28342).
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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 |
Apr
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
28
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pubmed:volume |
38
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1473-81
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:7739006-Animals,
pubmed-meshheading:7739006-Anti-Inflammatory Agents, Non-Steroidal,
pubmed-meshheading:7739006-Arthritis, Experimental,
pubmed-meshheading:7739006-Female,
pubmed-meshheading:7739006-Male,
pubmed-meshheading:7739006-Quinolines,
pubmed-meshheading:7739006-Rats,
pubmed-meshheading:7739006-Rats, Inbred Lew,
pubmed-meshheading:7739006-Rats, Sprague-Dawley,
pubmed-meshheading:7739006-Rats, Wistar
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pubmed:year |
1995
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pubmed:articleTitle |
Synthesis and antiinflammatory activity of certain 5,6,7,8-tetrahydroquinolines and related compounds.
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pubmed:affiliation |
Department of Medicinal Chemistry, Wyeth Research (U.K.) Ltd., Taplow, Maidenhead, Berkshire, United Kingdom.
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pubmed:publicationType |
Journal Article
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