Source:http://linkedlifedata.com/resource/pubmed/id/18164199
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
3
|
| pubmed:dateCreated |
2008-2-5
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| pubmed:abstractText |
This report describes replacement of the 4-(4-fluorophenyl)piperidine moiety in our CCR2 antagonists with 4-heteroaryl piperidine and 4-(carboxyphenyl)-piperidine subunits. Some of the resulting analogs retained potency in our CCR2 binding assay and had improved selectivity versus the I(Kr) channel; poor selectivity against I(Kr) had been a liability of earlier analogs in this series.
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| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Feb
|
| pubmed:issn |
1464-3405
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| pubmed:author | |
| pubmed:issnType |
Electronic
|
| pubmed:day |
1
|
| pubmed:volume |
18
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
994-8
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| pubmed:meshHeading |
pubmed-meshheading:18164199-Animals,
pubmed-meshheading:18164199-Humans,
pubmed-meshheading:18164199-Molecular Structure,
pubmed-meshheading:18164199-Piperidines,
pubmed-meshheading:18164199-Potassium Channel Blockers,
pubmed-meshheading:18164199-Rats,
pubmed-meshheading:18164199-Receptors, CCR2,
pubmed-meshheading:18164199-Structure-Activity Relationship
|
| pubmed:year |
2008
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| pubmed:articleTitle |
Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists.
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| pubmed:affiliation |
Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, 126 East Lincoln Avenue, Rahway, NJ 07065, USA. alexander_pasternak@merck.com
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| pubmed:publicationType |
Journal Article
|