Article ; Online: Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator.
Bioorganic & medicinal chemistry letters
2012 Volume 22, Issue 18, Page(s) 5936–5941
Abstract: A high-throughput screen utilizing a depolarization-triggered thallium influx through KCNQ1 channels was developed and used to screen the MLSMR collection of over 300,000 compounds. An iterative medicinal chemistry approach was initiated and from this ... ...
Abstract | A high-throughput screen utilizing a depolarization-triggered thallium influx through KCNQ1 channels was developed and used to screen the MLSMR collection of over 300,000 compounds. An iterative medicinal chemistry approach was initiated and from this effort, ML277 was identified as a potent activator of KCNQ1 channels (EC(50)=260 nM). ML277 was shown to be highly selective against other KCNQ channels (>100-fold selectivity versus KCNQ2 and KCNQ4) as well as against the distantly related hERG potassium channel. |
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MeSH term(s) | Animals ; Dose-Response Relationship, Drug ; Humans ; KCNQ1 Potassium Channel/agonists ; KCNQ1 Potassium Channel/metabolism ; Molecular Structure ; Piperidines/chemical synthesis ; Piperidines/chemistry ; Piperidines/pharmacology ; Rats ; Structure-Activity Relationship ; Substrate Specificity ; Thiazoles/chemical synthesis ; Thiazoles/chemistry ; Thiazoles/pharmacology ; Tosyl Compounds/chemical synthesis ; Tosyl Compounds/chemistry ; Tosyl Compounds/pharmacology |
Chemical Substances | (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide ; KCNQ1 Potassium Channel ; Piperidines ; Thiazoles ; Tosyl Compounds |
Language | English |
Publishing date | 2012-08-02 |
Publishing country | England |
Document type | Journal Article ; Research Support, N.I.H., Extramural |
ZDB-ID | 1063195-1 |
ISSN | 1464-3405 ; 0960-894X |
ISSN (online) | 1464-3405 |
ISSN | 0960-894X |
DOI | 10.1016/j.bmcl.2012.07.060 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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