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

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Jelena Penjisevic
Vladimir Sukalovic
Deana Andric
Goran Roglic
Irena Novakovic
Vukic Soskic
Sladjana Kostic-Rajacic

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-ylmethyl)piperazine. Biological evaluation of the synthesized compounds was pointed out seven compounds, of which 1-(2-methoxyphenyl)-4-{[1-(2-nitrobenzyl)piperidin-4-yl]methyl}piperazine has 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.

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How to Cite
[1]
J. Penjisevic, “Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines”, J. Serb. Chem. Soc., vol. 81, no. 4, pp. 347–356, May 2016.
Section
Organic Chemistry
Author Biographies

Jelena Penjisevic, ICTM – Center of Chemistry University of Belgrade

Center of Chemistry, Research Assistant

Vladimir Sukalovic, ICTM – Center of Chemistry University of Belgrade

Center of Chemistry, Assistant Research Professor

Deana Andric, Faculty of Chemistry University of Belgrade

Organic Chemistry Department, Associate Professor

Goran Roglic, Faculty of Chemistry University of Belgrade

Applied Chemistry Department, Associate Professor

Irena Novakovic, ICTM – Center of Chemistry University of Belgrade

Center of Chemistry, Assistant Research Professor

Vukic Soskic, ORGENTEC Diagnostica Gmbh

ORGENTEC Diagnostica Gmbh

Sladjana Kostic-Rajacic, ICTM – Center of Chemistry University of Belgrade

Center of Chemistry, Full Research Professor

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