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 |
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Hauptverfasser: | , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
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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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2007.10.114 |