Synthesis, biological evaluation, and docking studies of tetrahydrofuran-cyclopentanone-and cyclopentanol-based ligands acting at adrenergic α1-and serotonine 5- …

…, E Cichero, G Marucci, M Buccioni, A Cilia…

Index: Prandi, Adolfo; Franchini, Silvia; Manasieva, Leda Ivanova; Fossa, Paola; Cichero, Elena; Marucci, Gabriella; Buccioni, Michela; Cilia, Antonio; Pirona, Lorenza; Brasili, Livio Journal of Medicinal Chemistry, 2012 , vol. 55, # 1 p. 23 - 36

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Citation Number: 18

Abstract

A series of aralkylphenoxyethylamine and aralkylmethoxyphenylpiperazine compounds was synthesized and their in vitro pharmacological profile at both 5-HT1A receptors and α1- adrenoceptor subtypes was measured by binding assay and functional studies. The results showed that the replacement of the 1, 3-dioxolane ring by a tetrahydrofuran, cyclopentanone, or cyclopentanol moiety leads to an overall reduction of in vitro affinity at ...