Synthesis and evaluation of diphenylphosphinic amides and diphenylphosphine oxides as inhibitors of Kv1.5

Diphenylphosphinic amides and diphenylphosphine oxides have been synthesized and tested as inhibitors of the Kv1.5 potassium ion channel as a possible treatment for atrial fibrillation. In vitro structure–activity relationships are discussed and several compounds with Kv1.5 IC50 values of

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-02, Vol.23 (3), p.706-710
Hauptverfasser:	Olsson, Roine I., Jacobson, Ingemar, Boström, Jonas, Fex, Tomas, Björe, Annika, Olsson, Christina, Sundell, Johan, Gran, Ulrik, Öhrn, Anna, Nordin, Andreas, Gyll, Jonna, Thorstensson, Maria, Hayen, Ahlke, Aplander, Karolina, Hidestål, Olle, Jiang, Fanyi, Linhardt, Gunilla, Forsström, Elin, Collins, Teresa, Sundqvist, Monika, Lindhardt, Emma, Åstrand, Annika, Löfberg, Boel
Format:	Artikel
Sprache:	eng
Schlagworte:	amides Amides - chemical synthesis Amides - chemistry Amides - pharmacology Animals Atrial fibrillation Biphenyl Compounds - chemistry Diphenylphosphine oxides Diphenylphosphinic amides Fibrillation Humans IKs Inhibitory Concentration 50 ion channels Kv1.5 Kv1.5 Potassium Channel - antagonists & inhibitors Molecular Structure oxides Oxides - chemical synthesis Oxides - chemistry Oxides - pharmacology Phosphines - chemical synthesis Phosphines - chemistry Phosphines - pharmacology Phosphinic Acids - chemistry potassium Protein Binding - drug effects Rabbits Structure-Activity Relationship structure-activity relationships
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Zusammenfassung:	Diphenylphosphinic amides and diphenylphosphine oxides have been synthesized and tested as inhibitors of the Kv1.5 potassium ion channel as a possible treatment for atrial fibrillation. In vitro structure–activity relationships are discussed and several compounds with Kv1.5 IC50 values of
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.11.098