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Bioorg Med Chem Lett. 2014 Sep 15;24(18):4598-4602. doi: 10.1016/j.bmcl.2014.06.083. Epub 2014 Jul 5.

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

Author information

1
Drug Discovery Laboratory AS, Oslo Innovation Center, N-0349 Oslo, Norway; Department of Medicinal Chemistry, School of Pharmacy, University of Oslo, PO Box 1068 Blindern, N-0316 Oslo, Norway.
2
Department of Pharmacology, Faculty of Medicine, University of Oslo and Oslo University Hospital, PO Box 1057 Blindern, N-0316 Oslo, Norway; Department of Medicinal Chemistry, School of Pharmacy, University of Oslo, PO Box 1068 Blindern, N-0316 Oslo, Norway.
3
Department of Pharmacology, Faculty of Medicine, University of Oslo and Oslo University Hospital, PO Box 1057 Blindern, N-0316 Oslo, Norway; K.G. Jebsen Cardiac Research Centre and Center for Heart Failure Research, Faculty of Medicine, University of Oslo, Norway.
4
Drug Discovery Laboratory AS, Oslo Innovation Center, N-0349 Oslo, Norway.
5
Department of Medicinal Chemistry, School of Pharmacy, University of Oslo, PO Box 1068 Blindern, N-0316 Oslo, Norway. Electronic address: jo.klaveness@farmasi.uio.no.

Abstract

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.

KEYWORDS:

5-HT(4) receptor antagonists; Pharmacokinetic; hERG

PMID:
25149506
DOI:
10.1016/j.bmcl.2014.06.083
[Indexed for MEDLINE]

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