Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/4561
Title: Synthesis and biological activity of new 1,4-benzodioxan-arylpiperazine derivatives. Further validation of a pharmacophore model for alpha(1)-adrenoceptor antagonists
Authors: Barbaro, Roberta
Betti, Laura
Botta, Maurizio 
Corelli, Federico 
Giannaccini, Gino
Maccari, Laura
Manetti, Fabrizio 
Strappaghetti, Giovannella
Corsano, Stefano
Issue Date: 2002
Project: None 
Journal: BIOORGANIC & MEDICINAL CHEMISTRY
Abstract: 
A series of WB4101 (1)-related benzodioxanes (2-17) have been synthesized by replacing the phenoxyethyl moiety of 1 with a N-alkyl piperazine bearing a cyclic substituent (a substituted or unsubstituted phenyl group, a pyridine or pyridazinone ring, a furoyl moiety) at the second nitrogen atom. The binding profile of these compounds has been assessed by radioligand receptor binding assay at alpha(1)- and alpha(2)-adrenoceptors, in comparison to prazosin and rauwolscine, respectively. Moreover, structure-activity relationships have been derived for compounds 2-17 based on their fitting to a pharmacophore model for alpha(1)-adrenoceptor antagonists recently proposed by our research group. In a parallel way, the same compounds have been used to further test the predictive power and statistical significance of the model itself. The accuracy of the results obtained also in this case revealed the robustness of the calculated pharmacophore model and led to the identification of the molecular structural moieties which are thought to contribute to the biological activity.
Description: 
44546
URI: http://hdl.handle.net/20.500.12779/4561
ISSN: 0968-0896
Appears in Collections:Publications

Show full item record

Page view(s)

1
Last Week
0
Last month
1
checked on May 8, 2021

Google ScholarTM

Check


Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.