|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
2
|
|
pubmed:dateCreated |
2010-2-3
|
|
pubmed:abstractText |
A series of 1-(3-aryloxyaryl)benzimidazoles incorporating a sulfone substituent (6) was prepared. High affinity LXR ligands were identified (LXRbeta binding IC(50) values <10nM), some with excellent agonist potency and efficacy in a functional assay of LXR activity measuring ABCA1 mRNA increases in human macrophage THP1 cells. The compounds were typically stable in liver microsome preparations and had good oral exposure in mice.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Jan
|
|
pubmed:issn |
1464-3405
|
|
pubmed:author |
|
|
pubmed:copyrightInfo |
Copyright 2009 Elsevier Ltd. All rights reserved.
|
|
pubmed:issnType |
Electronic
|
|
pubmed:day |
15
|
|
pubmed:volume |
20
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
526-30
|
|
pubmed:meshHeading |
pubmed-meshheading:20006495-ATP-Binding Cassette Transporters,
pubmed-meshheading:20006495-Animals,
pubmed-meshheading:20006495-Benzimidazoles,
pubmed-meshheading:20006495-Cell Line,
pubmed-meshheading:20006495-Humans,
pubmed-meshheading:20006495-Mice,
pubmed-meshheading:20006495-Microsomes, Liver,
pubmed-meshheading:20006495-Orphan Nuclear Receptors,
pubmed-meshheading:20006495-RNA, Messenger,
pubmed-meshheading:20006495-Rats,
pubmed-meshheading:20006495-Structure-Activity Relationship,
pubmed-meshheading:20006495-Sulfones
|
|
pubmed:year |
2010
|
|
pubmed:articleTitle |
1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.
|
|
pubmed:affiliation |
Chemical Sciences, Wyeth Pharmaceuticals, 500 Arcola Road, Collegeville, PA 19426, USA.
|
|
pubmed:publicationType |
Journal Article
|
