Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
11
pubmed:dateCreated
1980-6-16
pubmed:abstractText
As part of continued efforts in the synthesis of structurally novel corticosteroids, a number of 17 alpha-benzoylated, 7 alpha-halogeno substituted prednisolones were tested for topical antiinflammatory activity. 7 alpha-Chloro, 7 alpha-bromo, and 7 alpha-iodo corticosteroids were synthesized by hydrogen halide addition to 1,4,6-triene-3-ones. The 7 alpha-fluoro substituted steroid was obtained by reaction of the appropriate 7 beta-hydroxy compound with N,N-diethyl(2-chloro-1,1,2-trifluoroethyl)amine. Antiinflammatory potencies were obtained using a croton oil-induced inflammation in the ears of mice. In this assay the greatest effect of a 7 alpha-halogen was observed in the 16 alpha-methylprednisolone series, where 7 alpha-fluoro and 7 alpha-bromo substitution yielded corticosteroids with topical potencies significantly higher than those of the corresponding 17,21-dipropionate analogs. Surprisingly, little potency enhancement due to 7 alpha-halogenation was discerned in the 16 beta-methylprednisolone series.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0004-4172
pubmed:author
pubmed:issnType
Print
pubmed:volume
29
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1662-7
pubmed:dateRevised
2008-11-21
pubmed:meshHeading
pubmed:year
1979
pubmed:articleTitle
A novel class of potent topical antiinflammatory agents: 17-benzoylated, 7 alpha-halogeno substituted corticosteroids.
pubmed:publicationType
Journal Article