Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5990
Title: Non-peptide NK1 receptor ligands based on the 4-phenylpyridine moiety.
Authors: Giuliani, Germano 
Cappelli, Andrea 
M., Matarrese
V., Masiello
E. A., Turolla
C., Monterisi
F., Fazio
Anzini, Maurizio 
G., PERICOT MOHR
D., Riitano
Finetti, Federica 
Morbidelli, Lucia
Ziche, Marina
Giorgi, Gianluca 
Vomero, Salvatore
Issue Date: 2011
Project: None 
Journal: BIOORGANIC & MEDICINAL CHEMISTRY
Abstract: 
The quinoline nucleus of the previously described 4-phenylquinoline-3-carboxamides NK(1) receptor ligands 7 has been transformed into either substituted or azole-(i.e., triazole or tetrazole) fused pyridine moieties of compounds 9 and 10, respectively, in order to obtain NK(1) receptor ligands showing lower molecular weight or higher hydrophilicity. The program of molecular manipulations produced NK(1) receptor ligands showing affinity in the nanomolar range. In particular, 4-methyl-1-piperazinyl derivative 9j showed an IC(50) value of 4.8 nM and was proved to behave as a NK(1) antagonist blocking Sar(9)-SP-sulfone induced proliferation and migration of microvascular endothelial cells. Therefore, compound 9j has been labeled with [(11)C]CH(3)I (t(1/2)=20.4 min, β(+)=99.8%) starting from the corresponding des-methyl precursor 9i using with a radiochemical yield of about 10% (not decay corrected) and a specific radioactivity>1 Ci/μmol in order to be used as a radiotracer in next PET studies.
Description: 
37015
URI: http://hdl.handle.net/20.500.12779/5990
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2011.02.031
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