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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4-6
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pubmed:dateCreated |
1988-2-25
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pubmed:abstractText |
The effect of various heteroaroyl groups in the 17-position of topical corticosteroids has been studied. The corticosteroids esterified at C17 were of 9 alpha,11 beta-dichloro, 9 alpha-chloro 11 beta-hydroxy and 9 alpha-fluoro 11 beta-hydroxy series. Among the 17-acyl groups 2'-furoates were most extensively investigated, although 2'-thenoates, 3'-thenoates and 3'-furoates were also examined. Many of these esters exhibited enhanced topical anti-inflammatory potencies. The most potent compounds investigated were the 21-chloro 17(2'-furoates) either in the 9 alpha,11 beta-dichloro, or in the 9 alpha-chloro 11 beta-hydroxy series. These compounds were at least 6 times as potent as betamethasone 17-valerate. Among 16-substituents studied 16 alpha-methyl compounds had the highest potency. Topical anti-inflammatory potencies were determined by using a 5-day modification of the croton oil ear assay in mice. The more potent compounds were also evaluated in the P. ovale induced chronic psoriaform lesion in the guinea-pig.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:issn |
0022-4731
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pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
27
|
pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
837-43
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:3695507-Administration, Topical,
pubmed-meshheading:3695507-Adrenal Cortex Hormones,
pubmed-meshheading:3695507-Animals,
pubmed-meshheading:3695507-Anti-Inflammatory Agents,
pubmed-meshheading:3695507-Carboxylic Acids,
pubmed-meshheading:3695507-Chemical Phenomena,
pubmed-meshheading:3695507-Chemistry,
pubmed-meshheading:3695507-Croton Oil,
pubmed-meshheading:3695507-Guinea Pigs,
pubmed-meshheading:3695507-Inflammation,
pubmed-meshheading:3695507-Mice,
pubmed-meshheading:3695507-Psoriasis,
pubmed-meshheading:3695507-Structure-Activity Relationship,
pubmed-meshheading:3695507-Tinea Versicolor
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pubmed:year |
1987
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pubmed:articleTitle |
Structure-activity relationships of a series of novel topical corticosteroids.
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pubmed:affiliation |
Pharmaceutical Research Division, Schering-Plough Corporation, Bloomfield, NJ 07003.
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pubmed:publicationType |
Journal Article,
Comparative Study
|