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

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Authors
Penjišević, Jelena
Šukalović, Vladimir
Andrić, Deana
Roglić, Goran
Novaković, Irena
Šoškić, Vukić
Kostić Rajačić, Slađana
Article (Published version)
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Abstract
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 site
Source:
Journal of the Serbian Chemical Society, 2016, 81, 4, 347-356
Publisher:
  • Serbian Chemical Soc, Belgrade
Projects:
  • Structure-activity relationship of newly synthesized biological active compound (RS-172032)

DOI: 10.2298/JSC151021097P

ISSN: 0352-5139

WoS: 000376210800001

Scopus: 2-s2.0-84971612072
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URI
http://cer.ihtm.bg.ac.rs/handle/123456789/2017
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