3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors

Lovell, Peter J., Blaney, Frank E., Goodacre, Caroline J., Scott, Claire M., Smith, Paul W., Starr, Kathryn R., Thewlis, Kevin M., Vong, Antonio K.K., Ward, Simon ORCID: https://orcid.org/0000-0002-8745-8377 and Watson, Jeannette M. 2006. 3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors. Bioorganic and Medicinal Chemistry Letters 17 (4) , pp. 1033-1036. 10.1016/j.bmcl.2006.11.031

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Abstract

Investigation of halogen substitution in lead compound 1 has led to the identification of analogues which combine high affinity for 5-HT1A receptors and potent serotonin reuptake inhibitory activity. Several compounds show an improved selectivity over 5-HT1B and 5-HT1D receptors and a superior pharmacokinetic profile in the rat.

Item Type:	Article
Date Type:	Published Online
Status:	Published
Schools:	Medicine
Uncontrolled Keywords:	5-HT1A, SSRI, Benzoxazinone
Publisher:	Elsevier
ISSN:	0960-894X
Date of Acceptance:	12 November 2006
Last Modified:	23 Oct 2022 13:01
URI:	https://orca.cardiff.ac.uk/id/eprint/109405

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