139153-32-5Relevant articles and documents
ARYLALKYLPIPERAZINES FOR USE AS NEUROPROTECTIVE AGENTS
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Page/Page column 30, (2016/07/05)
A compound of the general formula A or a or a pharmaceutically acceptable salt or solvate thereof, wherein: R1 is selected from the group consisting of: C1-C12-alkyl, C3-C12-cycloalkyl, C6-
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 D2 and 5-hydroxytryptamine 5HT1A receptors
Sukalovic, Vladimir,Ignjatovic, Djurdjica,Tovilovic, Gordana,Andric, Deana,Shakib, Kaveh,Kostic-Rajacic, Sladjana,Soskic, Vukic
scheme or table, p. 3967 - 3972 (2012/07/03)
It is suggested that the ratio of dopamine D2 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 D2 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-HT 1A receptors.