title: Novel selective and potent 5-HT reuptake inhibitors with 5-HT1D antagonist activity: chemistry and pharmacological evaluation of a series of thienopyran derivatives.
abstract: A series of compounds combining the naphthylpiperazine and thienopyran scaffolds has been prepared and evaluated for 5-HT reuptake inhibition with 5-HT1D antagonist activity. The design of these compounds has been based on the 'overlapping type' strategy where two pharmacophores are linked in a single molecule. The resultant dual pharmacological profile has the potential to deliver a more efficient treatment for depression.
authors.affiliation: Lilly, S. A., Avenida de la Industria, 30, 28108 Alcobendas, Madrid, Spain. torrado_alicia@lilly.com
authors.forename: Alicia
authors.initials: A
authors.lastname: Torrado
authors.forename: Carlos
authors.initials: C
authors.lastname: Lamas
authors.forename: Javier
authors.initials: J
authors.lastname: Agejas
authors.forename: Alma
authors.initials: A
authors.lastname: Jiménez
authors.forename: Nuria
authors.initials: N
authors.lastname: Diaz
authors.forename: Jeremy
authors.initials: J
authors.lastname: Gilmore
authors.forename: John
authors.initials: J
authors.lastname: Boot
authors.forename: Jeremy
authors.initials: J
authors.lastname: Findlay
authors.forename: Lorna
authors.initials: L
authors.lastname: Hayhurst
authors.forename: Louise
authors.initials: L
authors.lastname: Wallace
authors.forename: Richard
authors.initials: R
authors.lastname: Broadmore
authors.forename: Rosemarie
authors.initials: R
authors.lastname: Tomlinson
mesh_terms: D000818:Animals; D006801:Humans; D011714:Pyrans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D058829:Serotonin 5-HT1 Receptor Antagonists; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D011714:Pyrans; D058829:Serotonin 5-HT1 Receptor Antagonists; D012702:Serotonin Antagonists; D017367:Selective Serotonin Reuptake Inhibitors