Naphthyl piperazines with dual activity as 5-HT 1D antagonists and 5-HT reuptake inhibitors

• Published in: Bioorganic & medicinal chemistry letters Vol. 17; no. 12; pp. 3344 - 3348
• Main Authors: Bueno, Ana B., Gilmore, Jeremy, Boot, John, Broadmore, Richard, Cooper, Jane, Findlay, Jeremy, Hayhurst, Lorna, Marcos, Alicia, Montero, Carlos, Mitchell, Stephen, Timms, Graham, Tomlinson, Rosemarie, Wallace, Louise, Walton, Leslie
• Format: Journal Article
• Language: English
• Published: Elsevier Ltd 2007
• Subjects: 5-HT 1D antagonist; Serotonin reuptake inhibitor; 5-HT 1D antagonist; Serotonin reuptake inhibitor
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2007.03.101

A series of compounds with dual activity as 5-HT 1D antagonists and 5-HT reuptake inhibitors were prepared by incorporating naphthylpiperazines to substituted isochromans and dihydroisobenzofurans. 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, α 1, and D 2).