Naphthyl piperazines with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors

Ana B Bueno; Jeremy Gilmore; John Boot; Richard Broadmore; Jane Cooper; Jeremy Findlay; Lorna Hayhurst; Alicia Marcos; Carlos Montero; Stephen Mitchell; Graham Timms; Rosemarie Tomlinson; Louise Wallace; Leslie Walton

doi:10.1016/j.bmcl.2007.03.101

Naphthyl piperazines with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3344-8. doi: 10.1016/j.bmcl.2007.03.101. Epub 2007 Apr 5.

Authors

Ana B Bueno¹, Jeremy Gilmore, John Boot, Richard Broadmore, Jane Cooper, Jeremy Findlay, Lorna Hayhurst, Alicia Marcos, Carlos Montero, Stephen Mitchell, Graham Timms, Rosemarie Tomlinson, Louise Wallace, Leslie Walton

Affiliation

¹ Lilly SA, Avda. de la Industria, 30, 28108, Alcobendas, Madrid, Spain. [email protected]

PMID: 17434731
DOI: 10.1016/j.bmcl.2007.03.101

Abstract

SAR around a known molecule with dual 5-HT(1D) antagonist and 5-HT(transporter) inhibitory activity has led to the discovery of molecules with improved dual activity and reduced cross-reactivity toward other aminergic receptors (5-HT(1B), alpha(1), and D(2)).

MeSH terms

Animals
Antidepressive Agents / chemical synthesis
Antidepressive Agents / pharmacology*
Dose-Response Relationship, Drug
Guinea Pigs
Kinetics
Models, Chemical
Naphthalenes / chemistry*
Piperazines / chemical synthesis
Piperazines / pharmacology*
Receptor, Serotonin, 5-HT1D / drug effects*
Receptor, Serotonin, 5-HT1D / metabolism
Selective Serotonin Reuptake Inhibitors / chemical synthesis
Selective Serotonin Reuptake Inhibitors / pharmacology*
Serotonin Antagonists / chemical synthesis
Serotonin Antagonists / pharmacology*
Stereoisomerism
Structure-Activity Relationship

Substances

Antidepressive Agents
Naphthalenes
Piperazines
Receptor, Serotonin, 5-HT1D
Serotonin Antagonists
Serotonin Uptake Inhibitors