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)
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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
Funding / projects:
DOI: 10.2298/JSC151021097P
ISSN: 0352-5139
WoS: 000376210800001
Scopus: 2-s2.0-84971612072
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IHTMTY - JOUR AU - Penjišević, Jelena AU - Šukalović, Vladimir AU - Andrić, Deana AU - Roglić, Goran AU - Novaković, Irena AU - Šoškić, Vukić AU - Kostić Rajačić, Slađana PY - 2016 UR - https://cer.ihtm.bg.ac.rs/handle/123456789/2017 AB - 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. PB - Serbian Chemical Soc, Belgrade T2 - Journal of the Serbian Chemical Society T1 - Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines VL - 81 IS - 4 SP - 347 EP - 356 DO - 10.2298/JSC151021097P ER -
@article{ author = "Penjišević, Jelena and Šukalović, Vladimir and Andrić, Deana and Roglić, Goran and Novaković, Irena and Šoškić, Vukić and Kostić Rajačić, Slađana", year = "2016", 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.", publisher = "Serbian Chemical Soc, Belgrade", journal = "Journal of the Serbian Chemical Society", title = "Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines", volume = "81", number = "4", pages = "347-356", doi = "10.2298/JSC151021097P" }
Penjišević, J., Šukalović, V., Andrić, D., Roglić, G., Novaković, I., Šoškić, V.,& Kostić Rajačić, S.. (2016). Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines. in Journal of the Serbian Chemical Society Serbian Chemical Soc, Belgrade., 81(4), 347-356. https://doi.org/10.2298/JSC151021097P
Penjišević J, Šukalović V, Andrić D, Roglić G, Novaković I, Šoškić V, Kostić Rajačić S. Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines. in Journal of the Serbian Chemical Society. 2016;81(4):347-356. doi:10.2298/JSC151021097P .
Penjišević, Jelena, Šukalović, Vladimir, Andrić, Deana, Roglić, Goran, Novaković, Irena, Šoškić, Vukić, Kostić Rajačić, Slađana, "Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines" in Journal of the Serbian Chemical Society, 81, no. 4 (2016):347-356, https://doi.org/10.2298/JSC151021097P . .