N-{[2-(4-Phenyl-piperazin-1-yl)-ethyl]-phenyl}-arylamides with Dopamine D-2 and 5-Hydroxytryptamine 5HT(1A) Activity: Synthesis, Testing, and Molecular Modeling
2013
Аутори:
Šukalović, VladimirBogdan, Anca Elena
Tovilović-Kovačević, Gordana
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Ignjatović, Đurđica
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Andrić, Deana
Kostić-Rajačić, Slađana
Šoškić, Vukić
Тип документа:
Чланак у часопису (Објављена верзија)
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© 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Метаподаци
Приказ свих података о документуАпстракт:
The ratio of affinities toward the dopamine D-2 and the 5-hydroxytryptamine 5-HT1A receptors is one of the important parameters that determine the efficiency of antipsychotic drugs. Here, we present the synthesis of ortho-, meta-, and para-N-{[2-(4-phenyl-piperazin-1-yl)-ethyl]-phenyl}-arylamides and their structure-activity relationship studies on dopamine D-2 and 5-hydroxytryptamine 5-HT1A receptors. It was shown that the biological activity of the described ligands strongly depends on their topology as well as on the nature of the heteroaryl group in the head of the molecules. Docking simulations together with conformational analysis revealed a rational explanation for the ligands' behavior. The molecular model of receptor-ligand interactions described herein provided us with a tool for the rational design of new compounds with a favorable D-2/5-HT1A profile.
Кључне речи:
Arylpiperazine; Dopamine receptors; Serotonin receptorsИзвор:
Archiv der Pharmazie, 2013, 346, 10, 708-717Финансирање / пројекти:
- Проучавање односа структуре и активности новосинтетисаних биолошки активних супстанци (RS-MESTD-Basic Research (BR or ON)-172032)
DOI: 10.1002/ardp.201300189
ISSN: 0365-6233
PubMed: 24105736