Structure–affinity/activity relationships of 1,4-dioxa-spiro[4.5]decane based ligands at α 1 and 5-HT1A receptors

• Published in: European journal of medicinal chemistry Vol. 87; pp. 248 - 266
• Main Authors: Franchini, Silvia, Battisti, Umberto M., Baraldi, Annamaria, Prandi, Adolfo, Fossa, Paola, Cichero, Elena, Tait, Annalisa, Sorbi, Claudia, Marucci, Gabriella, Cilia, Antonio, Pirona, Lorenza, Brasili, Livio
• Format: Journal Article
• Language: English
• Published: Elsevier Masson SAS 24.11.2014
• Subjects: 1,3-Dioxolane; 5-HT1AR; Arylpiperazine derivatives; Structure–affinity/activity relationships; α 1 receptor; Arylpiperazine derivatives; Structure–affinity/activity relationships; 1,3-Dioxolane; α 1 receptor; 5-HT1AR

Recently, 1-(1,4-dioxaspiro[4,5]dec-2-ylmethyl)-4-(2-methoxyphenyl)piperazine (1) was reported as a highly selective and potent 5-HT1AR ligand. In the present work we adopted an in-parallel synthetic strategy to rapidly explore a new set of arylpiperazine (7–32) that is structurally related to 1. Th...