Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
|
pubmed:dateCreated |
1990-6-28
|
pubmed:abstractText |
A perception of structural similarities between two independent series of leukotriene antagonists (one emanating from FPL 55712 and one based upon the leukotrienes themselves) led to the discovery of a novel class of indole and indazole derived antagonists of peptidoleukotrienes. A systematic exploration of C-6 substituted 4-(indol-1-ylmethyl)-3-methoxybenzoic acids identified cyclopentylacetamide and cyclopentylurethane as preferred substituents. The corresponding indazoles were equipotent. These compounds are selective leukotriene antagonists with pKB values of 7.5-7.8 vs LTE4 on guinea pig trachea.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Jun
|
pubmed:issn |
0022-2623
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
33
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1771-81
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:2342071-Animals,
pubmed-meshheading:2342071-Guinea Pigs,
pubmed-meshheading:2342071-Indazoles,
pubmed-meshheading:2342071-Indoles,
pubmed-meshheading:2342071-Muscle Contraction,
pubmed-meshheading:2342071-Pyrazoles,
pubmed-meshheading:2342071-SRS-A,
pubmed-meshheading:2342071-Structure-Activity Relationship
|
pubmed:year |
1990
|
pubmed:articleTitle |
Evolution of a series of peptidoleukotriene antagonists: synthesis and structure-activity relationships of 1,6-disubstituted indoles and indazoles.
|
pubmed:affiliation |
Department of Medicinal Chemistry, ICI Pharmaceuticals Group, Wilmington, Delaware 19897.
|
pubmed:publicationType |
Journal Article,
In Vitro
|