Novel selective and potent 5-HT reuptake inhibitors with 5-HT1D antagonist activity: chemistry and pharmacological evaluation of a series of thienopyran derivatives.
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.
Torrado
Alicia
A
Lilly, S. A., Avenida de la Industria, 30, 28108 Alcobendas, Madrid, Spain. torrado_alicia@lilly.com
Lamas
Carlos
C
Agejas
Javier
J
Jiménez
Alma
A
Diaz
Nuria
N
Gilmore
Jeremy
J
Boot
John
J
Findlay
Jeremy
J
Hayhurst
Lorna
L
Wallace
Louise
L
Broadmore
Richard
R
Tomlinson
Rosemarie
R
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*
D011714:Pyrans; D058829:Serotonin 5-HT1 Receptor Antagonists; D012702:Serotonin Antagonists; D017367:Selective Serotonin Reuptake Inhibitors