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Interactions of N-{[2-(4-phenyl-piperazin-1-yl)-ethyl]-phenyl}-2-aryl-2-yl-acetamides and 1-{[2-(4-phenyl-piperazin-1-yl)-ethyl]-phenyl}-3-aryl-2-yl-ureas with dopamine D-2 and 5-hydroxytryptamine 5HT(1A) receptors

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2012
Authors
Šukalović, Vladimir
Ignjatović, Đurđica S.
Tovilović, Gordana
Andrić, Deana
Shakib, Kaveh
Kostić Rajačić, Slađana
Šoškić, Vukić
Article (Published version)
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Abstract
It is suggested that the ratio of dopamine D-2 to 5-hydroxytryptamine 5-HT1A activity is an important parameter that determines the efficiency of antipsychotic drugs. Here we present the synthesis of N-{[2-(4-phenyl-piperazin-1-yl)-ethyl]-phenyl}-2-aryl-2-yl-acetamides and 1-{[2-(4-phenyl-piperazin-1-yl)-ethyl]-phenyl}-3-aryl-2-yl-ureas and their structure-activity relationship studies on dopamine D-2 and 5-hydrohytryptamine 5-HT1A receptors. It was shown that ligand selectivity and affinity strongly depends on their topology and the presence of a pyridyl group in the head of molecules. Molecular modeling studies using homology modeling and docking simulation revealed a rational explanation for the ligand behavior. The observed binding modes and receptor-ligand interactions provided us with a clue for optimizing the optimal selectivity towards 5-HT1A receptors.
Keywords:
Dopamine / 5-Hydroxytryptamine / Receptor / Arylpiperazine / Molecular docking
Source:
Bioorganic and Medicinal Chemistry Letters, 2012, 22, 12, 3967-3972
Publisher:
  • Pergamon-Elsevier Science Ltd, Oxford
Projects:
  • Structure-activity relationship of newly synthesized biological active compound (RS-172032)

DOI: 10.1016/j.bmcl.2012.04.098

ISSN: 0960-894X

PubMed: 22607670

WoS: 000304484600023

Scopus: 2-s2.0-84861576055
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URI
http://cer.ihtm.bg.ac.rs/handle/123456789/974
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