Linked Life Data

3172130

Source:http://linkedlifedata.com/resource/pubmed/id/3172130

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
10
pubmed:dateCreated
1988-11-18
pubmed:abstractText
The nature of the carbonyl and nitrogen substituents of hydroxamic acids has a major influence on the biological profile of these compounds. Hydroxamates with small groups such as methyl appended to the carbonyl and relatively large nitrogen substituents generally have longer duration in vivo, produce greater plasma concentrations, and often are more potent inhibitors of in vivo leukotriene biosynthesis than hydroxamic acids with the opposite arrangement. The structure-activity relationships that describe in vitro 5-lipoxygenase inhibitory activity and in vivo leukotriene biosynthesis inhibitory potency for a group of these hydroxamic acids were investigated. While most of the compounds examined were potent in vitro inhibitors of 5-lipoxygenase, their in vivo potencies varied widely. This discrepancy was usually attributable to differences in bioavailability. Substitution patterns are described that produce potent, orally active inhibitors of leukotriene biosynthesis.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:volume
31
pubmed:owner
NLM
pubmed:authorsComplete
N
pubmed:pagination
1960-4
pubmed:dateRevised
2003-11-14
pubmed:meshHeading
pubmed:year
1988
pubmed:articleTitle
Structure-activity analysis of a class of orally active hydroxamic acid inhibitors of leukotriene biosynthesis.
pubmed:affiliation
Department 47K, Abbott Laboratories, Abbott Park, Illinois 60064.
pubmed:publicationType
Journal Article