Linked Life Data

8057289

Source:http://linkedlifedata.com/resource/pubmed/id/8057289

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
15
pubmed:dateCreated
1994-9-12
pubmed:abstractText
A series of (hydroxyphenyl)pyrazoles was designed by molecular modeling comparison with the LTB4 structure and prepared for evaluation as LTB4 receptor antagonists, culminating in 4-ethyl-5-[[6-methyl-6-(1H-tetrazol-5-yl)heptyl]oxy]-2-(1H-pyrazol -3- yl)phenol (2). Using an assay for inhibition of specific [3H]LTB4 binding to human PMN, it was found that the pyrazole ring could be methylated at N(1) with little loss of activity while methylation at N(2) reduced activity significantly. The structure-activity relationship of the terminal acid group was investigated. Good activity was found with o- and m-phenylalkanoic acids, chromane carboxylic acid, and tetrazole groups. The best in vitro activity was realized with the pyrazole nitrogen unsubstituted and with a six-carbon chain linking the phenyl ether oxygen to the tetrazole group. Compound 2, having an IC50 of 6.4 +/- 0.8 nM in the binding assay, was selected for further preclinical evaluation.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:day
22
pubmed:volume
37
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2411-20
pubmed:dateRevised
2004-11-17
pubmed:meshHeading
pubmed:year
1994
pubmed:articleTitle
Leukotriene B4 (LTB4) receptor antagonists: a series of (hydroxyphenyl)pyrazoles.
pubmed:affiliation
Lilly Research Laboratories, Eli Lilly & Company, Indianapolis, Indiana 46285.
pubmed:publicationType
Journal Article