|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0002482,
umls-concept:C0205314,
umls-concept:C0205460,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0439799,
umls-concept:C0679622,
umls-concept:C1416548,
umls-concept:C1552603,
umls-concept:C1706202,
umls-concept:C1883254
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|
pubmed:issue |
11
|
|
pubmed:dateCreated |
2004-5-5
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|
pubmed:abstractText |
The search for novel, potent Kv1.5 blockers based on an anthranilic amide scaffold employing a pharmacophore-based virtual screening approach is described. The synthesis and structure-activity relationships (SAR) with respect to inhibition of the Kv1.5 channel are discussed. The most potent compounds display sub-micromolar inhibition of Kv1.5 and no significant effect on the HERG channel. In addition, good oral bioavailability is demonstrated for compound 3i in rats.
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|
pubmed:language |
eng
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|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Jun
|
|
pubmed:issn |
0960-894X
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|
pubmed:author |
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
7
|
|
pubmed:volume |
14
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
2823-7
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|
pubmed:dateRevised |
2005-11-17
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|
pubmed:meshHeading |
pubmed-meshheading:15125940-Administration, Oral,
pubmed-meshheading:15125940-Amides,
pubmed-meshheading:15125940-Animals,
pubmed-meshheading:15125940-Anthranilic Acids,
pubmed-meshheading:15125940-Biological Availability,
pubmed-meshheading:15125940-Dose-Response Relationship, Drug,
pubmed-meshheading:15125940-Humans,
pubmed-meshheading:15125940-Inhibitory Concentration 50,
pubmed-meshheading:15125940-Kv1.5 Potassium Channel,
pubmed-meshheading:15125940-Models, Molecular,
pubmed-meshheading:15125940-Potassium Channel Blockers,
pubmed-meshheading:15125940-Potassium Channels, Voltage-Gated,
pubmed-meshheading:15125940-Rats,
pubmed-meshheading:15125940-Structure-Activity Relationship
|
|
pubmed:year |
2004
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|
pubmed:articleTitle |
Pharmacophore-based search, synthesis, and biological evaluation of anthranilic amides as novel blockers of the Kv1.5 channel.
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|
pubmed:affiliation |
Aventis Pharma Deutschland GmbH, Medicinal Chemistry and DG Cardiovascular, D-65926 Frankfurt, Germany. stefan.peukert@aventis.com
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pubmed:publicationType |
Journal Article
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