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Title: Design, Synthesis, and a1-Adrenoceptor Binding Properties of New Arylpiperazine Derivatives bearing a Flavone Nucleus as the Terminal Heterocyclic Molecular Portion
Authors: Betti, L.
Floridi, M.
Giannaccini, G.
Manetti, Fabrizio 
Paparelli, C.
Strappaghetti, G.
Botta, Maurizio 
Keywords: α1-Adrenoceptor affinity; Flavone; Pharmacophore; Pyridazinone-piperazine
Issue Date: 2004
Project: None 
Following our research project aimed at obtaining new compounds with high affinity and selectivity toward α1-adrenoceptors (AR), a new class of piperazine derivatives was designed, synthesized and biologically tested. The new compounds 1-13 are characterized by a flavone system linked, through an ethoxy or propoxy spacer, to a phenyl- or pyridazinone-piperazine moiety. Biological data showed an interesting profile for the phenylpiperazine subclass found to have a nanomolar affinity toward α1-AR, and less pronounced affinity for α2-AR and the 5-HT1A serotoninergic receptor. A discussion on the structure-activity relationship (SAR) of such compounds is also reported, on the basis of the flavone substitution pattern, length and functionalization of the spacer, and disruption of the phenylpiperazine system.
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2003.12.033
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