Linked Life Data

7894968

Source:http://linkedlifedata.com/resource/pubmed/id/7894968

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
8
pubmed:dateCreated
1995-4-21
pubmed:abstractText
A series of arylsulfonamido-substituted omega-phenyl-omega-(3-pyridyl)alkenoic acids were synthesized and evaluated in vitro for their ability to act as both a thromboxane A2 receptor antagonist (TRA) and thromboxane synthase inhibitor (TSI). Variations of alkenoic acid chain length, olefin geometry, substituent effect on the benzenesulfonamido group, and conformational flexibility of the substituted arylsulfonamido group were examined. Among the various substituents, iodo-substitution gave the most potent compound. Conformational flexibility between the arylsulfonamido group and the phenyl ring attached to the alkenoic acid side chain significantly enhanced the dual activities. The compound (E)-21c was identified as the most potent TRA/TSI (TRA: Kd = 53 nM; TSI: IC50 = 23 nM) in the series studied. The compounds 9c and 10c have indicated that these series of compounds are orally active and are specific TSIs as exhibited by the so-called 'shunt' effect on prostacyclin synthesis in vitro.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
0968-0896
pubmed:author
pubmed:issnType
Print
pubmed:volume
2
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
743-55
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1994
pubmed:articleTitle
Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition--I. Synthesis, structure-activity relationship, and evaluation of substituted omega-phenyl-omega-(3-pyridyl)alkenoic acids.
pubmed:affiliation
Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, Indiana 46285.
pubmed:publicationType
Journal Article, In Vitro