N-tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B

Yoon Jin Kwon; Simon Saubern; James M Macdonald; Xi-Ping Huang; Vincent Setola; Bryan L Roth

doi:10.1016/j.bmcl.2010.07.074

N-tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5488-90. doi: 10.1016/j.bmcl.2010.07.074. Epub 2010 Jul 21.

Authors

Yoon Jin Kwon¹, Simon Saubern, James M Macdonald, Xi-Ping Huang, Vincent Setola, Bryan L Roth

Affiliation

¹ CSIRO Molecular and Health Technologies, Bag 10, Clayton MDC, Clayton, VIC 3169, Australia.

PMID: 20692833
DOI: 10.1016/j.bmcl.2010.07.074

Abstract

The serendipitous discovery of N-cyclohexyl-8-fluoro-3,3a,4,9b-tetrahydro-1H-thiochromeno[4,3-c]isoxazole-1-carboxamide as a selective human serotonin 5-HT2B antagonist with Ki of 42+/-5 nM is reported herein. A subsequent functional assay indicated little agonist activity compared to 5-HT itself.

Publication types

Research Support, N.I.H., Extramural

MeSH terms

Heterocyclic Compounds, 3-Ring / chemistry*
Heterocyclic Compounds, 3-Ring / pharmacology*
Humans
Receptor, Serotonin, 5-HT2B / metabolism*
Serotonin 5-HT2 Receptor Antagonists / chemistry*
Serotonin 5-HT2 Receptor Antagonists / pharmacology*
Structure-Activity Relationship

Substances

Heterocyclic Compounds, 3-Ring
Receptor, Serotonin, 5-HT2B
Serotonin 5-HT2 Receptor Antagonists

Abstract

Publication types

MeSH terms

Substances

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