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

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-ylmethyl)piperazine. Biological evaluation of the synthesized c...

Full description

Bibliographic Details
Main Authors: Penjišević Jelena Z., Šukalović Vladimir V., Andrić Deana B., Roglić Goran M., Novaković Irena T., Šoškić Vukić, Kostić-Rajačić Slađana V.
Format: Article
Language:English
Published: Serbian Chemical Society 2016-01-01
Series:Journal of the Serbian Chemical Society
Subjects:
Online Access:http://www.doiserbia.nb.rs/img/doi/0352-5139/2016/0352-51391500097P.pdf
_version_ 1818645719231234048
author Penjišević Jelena Z.
Šukalović Vladimir V.
Andrić Deana B.
Roglić Goran M.
Novaković Irena T.
Šoškić Vukić
Kostić-Rajačić Slađana V.
author_facet Penjišević Jelena Z.
Šukalović Vladimir V.
Andrić Deana B.
Roglić Goran M.
Novaković Irena T.
Šoškić Vukić
Kostić-Rajačić Slađana V.
author_sort Penjišević Jelena Z.
collection DOAJ
description 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-ylmethyl)piperazine. Biological evaluation of the synthesized compounds was pointed out for seven compounds, of which 1-(2-methoxyphenyl)-4-{[1-(2-nitrobenzyl)piperidin-4-yl]methyl}piperazine had the highest affinity for the dopamine D2 receptor. For all seven selected compounds docking analysis was performed in order to establish their structure-to-activity relationship. [Projekat Ministarstva nauke Republike Srbije, br. 172032]
first_indexed 2024-12-17T00:35:13Z
format Article
id doaj.art-a7137916291b4b4397e62894eeef55e3
institution Directory Open Access Journal
issn 0352-5139
1820-7421
language English
last_indexed 2024-12-17T00:35:13Z
publishDate 2016-01-01
publisher Serbian Chemical Society
record_format Article
series Journal of the Serbian Chemical Society
spelling doaj.art-a7137916291b4b4397e62894eeef55e32022-12-21T22:10:10ZengSerbian Chemical SocietyJournal of the Serbian Chemical Society0352-51391820-74212016-01-0181434735610.2298/JSC151021097P0352-51391500097PSynthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazinesPenjišević Jelena Z.0Šukalović Vladimir V.1Andrić Deana B.2Roglić Goran M.3Novaković Irena T.4Šoškić Vukić5Kostić-Rajačić Slađana V.6ICTM - Center of Chemistry, BelgradeICTM - Center of Chemistry, BelgradeFaculty of Chemistry, BelgradeFaculty of Chemistry, BelgradeICTM - Center of Chemistry, BelgradeORGENTEC Diagnostica Gmbh, Mainz, GermanyICTM - Center of Chemistry, BelgradeA 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-ylmethyl)piperazine. Biological evaluation of the synthesized compounds was pointed out for seven compounds, of which 1-(2-methoxyphenyl)-4-{[1-(2-nitrobenzyl)piperidin-4-yl]methyl}piperazine had the highest affinity for the dopamine D2 receptor. For all seven selected compounds docking analysis was performed in order to establish their structure-to-activity relationship. [Projekat Ministarstva nauke Republike Srbije, br. 172032]http://www.doiserbia.nb.rs/img/doi/0352-5139/2016/0352-51391500097P.pdfdopamine D2 receptordocking analysisallostericorthosteric bind site
spellingShingle Penjišević Jelena Z.
Šukalović Vladimir V.
Andrić Deana B.
Roglić Goran M.
Novaković Irena T.
Šoškić Vukić
Kostić-Rajačić Slađana V.
Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines
Journal of the Serbian Chemical Society
dopamine D2 receptor
docking analysis
allosteric
orthosteric bind site
title Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines
title_full Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines
title_fullStr Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines
title_full_unstemmed Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines
title_short Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines
title_sort synthesis biological evaluation and docking analysis of substituted piperidines and 2 methoxyphenyl piperazines
topic dopamine D2 receptor
docking analysis
allosteric
orthosteric bind site
url http://www.doiserbia.nb.rs/img/doi/0352-5139/2016/0352-51391500097P.pdf
work_keys_str_mv AT penjisevicjelenaz synthesisbiologicalevaluationanddockinganalysisofsubstitutedpiperidinesand2methoxyphenylpiperazines
AT sukalovicvladimirv synthesisbiologicalevaluationanddockinganalysisofsubstitutedpiperidinesand2methoxyphenylpiperazines
AT andricdeanab synthesisbiologicalevaluationanddockinganalysisofsubstitutedpiperidinesand2methoxyphenylpiperazines
AT roglicgoranm synthesisbiologicalevaluationanddockinganalysisofsubstitutedpiperidinesand2methoxyphenylpiperazines
AT novakovicirenat synthesisbiologicalevaluationanddockinganalysisofsubstitutedpiperidinesand2methoxyphenylpiperazines
AT soskicvukic synthesisbiologicalevaluationanddockinganalysisofsubstitutedpiperidinesand2methoxyphenylpiperazines
AT kosticrajacicslađanav synthesisbiologicalevaluationanddockinganalysisofsubstitutedpiperidinesand2methoxyphenylpiperazines