Design, synthesis, pharmacological evaluation and computational studies of 1-(biphenyl-4-yl)-2-[4-(substituted phenyl)-piperazin-1-yl]ethanones as potential antipsychotics

Add time:07/12/2019    Source:sciencedirect.com

This article describes the design of biphenyl moiety linked with aryl piperazine and syntheses of fourteen 1-(biphenyl-4-yl)-2-[4-(substituted phenyl)-piperazin-1-yl]ethanone derivatives along with their pharmacological evaluation for antipsychotic activity and computational studies including quantitative structure activity relationship (QSAR) and descriptor based similarity study. All compounds were found to exhibit considerable anti-dopaminergic and anti-serotonergic activity in behavioural models. Among all derivatives, compound 1-(biphenyl-4-yl)-2-[4-(2-methoxyphenyl)-piperazin-1-yl]ethanone (3c) and 1-(biphenyl-4-yl)-2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]ethanone (3k) showed impressive antipsychotic profile with lower potency for catalepsy induction. These results were found to be sturdily matching with docking study in designing of compounds with homology model of human dopamine D2 receptor. Also the QSAR study strongly supports the obtained results.

We also recommend Trading Suppliers and Manufacturers of 2-(biphenyl-4-yl)-5,6,7,8-tetrahydro-1H-benzo[f]indole (cas 38824-46-3). Pls Click Website Link as below: cas 38824-46-3 suppliers

Prev:Theoretical investigation of the vibronic phosphorescence spectra and quantum yields for iridium(III) complexes with 2-(2,5,2′,3′,4′,5′,6′-heptafluoro-biphenyl-4-yl)-pyridine as the primary ligand
Next:Process Intensification of Tetrazole reaction through tritylation of 5-[4′-(Methyl) Biphenyl-2-Yl] using microreactors)