Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines

2016
Authors
Penjišević, Jelena
Šukalović, Vladimir

Andrić, Deana

Roglić, Goran

Novaković, Irena

Šoškić, Vukić

Kostić Rajačić, Slađana

Article (Published version)
Metadata
Show full item recordAbstract
A series of sixteen novel substituted piperidines and (2-methoxyphenyl)piperazines were synthesized, starting from the key intermediates 1-(2-methoxyphenyl)-4-(piperidin-4-yl)piperazine and 1-(2-methoxyphenyl)-4-[(piperidin-4-yl)methyl] piperazine. Biological evaluation of the synthesized compounds was illustrated by seven compounds, of which 1-(2-methoxyphenyl)-4-{[1-(2-nitrobenzyl) piperidin-4-yl] methyl} piperazine had the highest affinity for the dopamine D-2 receptor. For all seven selected compounds, docking analysis was performed in order to establish their structure-to-activity relationship.
Keywords:
dopamine D-2 receptor / docking analysis / allosteric / orthosteric binding siteSource:
Journal of the Serbian Chemical Society, 2016, 81, 4, 347-356Publisher:
- Serbian Chemical Soc, Belgrade
Projects:
DOI: 10.2298/JSC151021097P
ISSN: 0352-5139