Discovery and pharmacological profile of new hydrophilic 5-HT(4) receptor antagonists

The synthesis and pharmacological data of some new and potent hydrophilic 5-HT4 receptor antagonists are described. Propanediol derivative 25 was identified as a potent antagonist with low affinity for the hERG potassium channel and promising pharmacokinetics.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-09, Vol.24 (18), p.4598-4602
Hauptverfasser:	Brudeli, Bjarne, Navaratnarajah, Mirusha, Andressen, Kjetil Wessel, Manfra, Ornella, Moltzau, Lise Román, Nilsen, Nils Olav, Levy, Finn Olav, Klaveness, Jo
Format:	Artikel
Sprache:	eng
Schlagworte:	Dose-Response Relationship, Drug Drug Discovery Ether-A-Go-Go Potassium Channels - antagonists & inhibitors Ether-A-Go-Go Potassium Channels - metabolism Humans Hydrophobic and Hydrophilic Interactions Molecular Structure Propylene Glycols - chemical synthesis Propylene Glycols - chemistry Propylene Glycols - pharmacology Receptors, Serotonin, 5-HT4 - metabolism Serotonin 5-HT4 Receptor Antagonists - chemical synthesis Serotonin 5-HT4 Receptor Antagonists - chemistry Serotonin 5-HT4 Receptor Antagonists - pharmacology Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	The synthesis and pharmacological data of some new and potent hydrophilic 5-HT4 receptor antagonists are described. Propanediol derivative 25 was identified as a potent antagonist with low affinity for the hERG potassium channel and promising pharmacokinetics.
ISSN:	1464-3405
DOI:	10.1016/j.bmcl.2014.06.083