1369303-80-9Relevant articles and documents
Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure-Activity and Structure-Property Relationship Studies
Neelarapu, Raghupathi,Maignan, Jordany R.,Lichorowic, Cynthia L.,Monastyrskyi, Andrii,Mutka, Tina S.,LaCrue, Alexis N.,Blake, Lynn D.,Casandra, Debora,Mashkouri, Sherwin,Burrows, Jeremy N.,Willis, Paul A.,Kyle, Dennis E.,Manetsch, Roman
, p. 1450 - 1473 (2018/03/05)
Malaria deaths have been decreasing over the last 10-15 years, with global mortality rates having fallen by 47% since 2000. While the World Health Organization (WHO) recommends the use of artemisinin-based combination therapies (ACTs) to combat malaria, the emergence of artemisinin resistant strains underscores the need to develop new antimalarial drugs. Recent in vivo efficacy improvements of the historical antimalarial ICI 56,780 have been reported, however, with the poor solubility and rapid development of resistance, this compound requires further optimization. A series of piperazine-containing 4(1H)-quinolones with greatly enhanced solubility were developed utilizing structure-activity relationship (SAR) and structure-property relationship (SPR) studies. Furthermore, promising compounds were chosen for an in vivo scouting assay to narrow selection for testing in an in vivo Thompson test. Finally, two piperazine-containing 4(1H)-quinolones were curative in the conventional Thompson test and also displayed in vivo activity against the liver stages of the parasite.
Quinolone-based compounds, formulations, and uses thereof
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Page/Page column 60; 62, (2018/07/02)
Provided herein are quinolone-based compounds that can be used for treatment and/or prevention of malaria and formulations thereof. Also provided herein are methods of treating and/or preventing malaria in a subject by administering a quinolone-based compound or formulation thereof provided herein.
ARYLALKYLPIPERAZINES FOR USE AS NEUROPROTECTIVE AGENTS
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Page/Page column 29, (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
, 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.
ARYLPIPERAZINES AS NEUROPROTECTIVE AGENTS
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Page/Page column 20-21, (2012/10/08)
The present invention generally relates to novel arylpiperazines. In particular, these arylpiperazines can be used as neuroprotective agents. The invention also relates to a process for the manufacture of the novel compounds. Further, the invention relates to the use of the novel arylpiperazines in the treatment of diseases associated with, accompanied by or caused by mitochondrial stress.