Sulfonate chalcone as new class voltage-dependent K + channel blocker

Sulfonate Chalcones 9– 17 were found to exhibit the potential to act as a new class of voltage-dependent K + channel blockers. Chalcone derivatives 1– 17 were synthesized and their voltage-dependent K + channel inhibitory activities were investigated. The effective K + channel blockers were shown to...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2008, Vol.18 (1), p.137-140
Hauptverfasser: Yarishkin, Oleg V., Ryu, Hyung Won, Park, Jae-Yong, Yang, Min Suk, Hong, Seong-Geun, Park, Ki Hun
Format: Artikel
Sprache:eng
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Zusammenfassung:Sulfonate Chalcones 9– 17 were found to exhibit the potential to act as a new class of voltage-dependent K + channel blockers. Chalcone derivatives 1– 17 were synthesized and their voltage-dependent K + channel inhibitory activities were investigated. The effective K + channel blockers were shown to be sulfonate chalcones 9– 17, in which the sulfonyloxy group is placed on the A-ring. The 3′-( p-aminobenzene-sulfonylhydroxy)-4-hydroxychalcone 17 (IC 50 = 0.51 ± 0.05 μM) was the most potent K + channel blocker.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.10.114