Full metadata record
DC Field | Value | Language |
---|---|---|
dc.creator | Mendoza, A. (Adela) | - |
dc.creator | Pérez-Silanes, S. (Silvia) | - |
dc.creator | Quiliano, M. (Miguel) | - |
dc.creator | Pabon, A. (Adriana) | - |
dc.creator | Gonzalez, G. (Germán) | - |
dc.creator | Garavito, G. (Giovanny) | - |
dc.creator | Zimic, M. (Mirko) | - |
dc.creator | Vaisberg, A. (Abrahm) | - |
dc.creator | Aldana, I. (Ignacio) | - |
dc.creator | Monge, A. (Antonio) | - |
dc.creator | Deharo, E. (Eric) | - |
dc.date.accessioned | 2011-07-04T17:59:16Z | - |
dc.date.available | 2011-07-04T17:59:16Z | - |
dc.date.issued | 2011 | - |
dc.identifier.citation | Mendoza A, Perez-Silanes S, Quiliano M, Pabon A, Galiano S, Gonzalez G, et al. Aryl piperazine and pyrrolidine as antimalarial agents. Synthesis and investigation of structure-activity relationships. Exp Parasitol 2011 Jun;128(2):97-103. | es_ES |
dc.identifier.issn | 0014-4894 | - |
dc.identifier.uri | https://hdl.handle.net/10171/18730 | - |
dc.description.abstract | Piperazine and pyrrolidine derivatives were synthesized and evaluated for their capacity to inhibit the growth of Plasmodium falciparum chloroquine-resistant (FCR-3) strain in culture. The combined presence of a hydroxyl group, a propane chain and a fluor were shown to be crucial for the antiplasmodial activity. Five compounds of the aryl-alcohol series inhibited 50% of parasite growth at doses ≤ 10 µM. The most active compound 1-(4-fluoronaphthyl)-3-[4-(4-nitro-2-trifluoromethylphenyl)piperazin-1-yl]propan-1-ol was almost 20 to 40 times more active on Plasmodium falciparum (IC50: 0.5 µM) than on tumorogenic and non tumorogenic cells. Calculated physicochemical parameters showed a good potential for intestinal absorption, but due to difficulty in being solubilised prior to oral administration, it was weakly active against Plasmodium berghei infected mice (ED50: 35%). In silico molecular docking study and molecular electrostatic potential calculation revealed that this compound bound to the active site of Plasmodium plasmepsin II enzyme. | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | Elsevier | es_ES |
dc.rights | info:eu-repo/semantics/openAccess | es_ES |
dc.subject | Piperazine | es_ES |
dc.subject | Pyrrolidine | es_ES |
dc.subject | Antiplasmodial | es_ES |
dc.subject | Plasmodium | es_ES |
dc.subject | Antimalarial agents | es_ES |
dc.subject | Docking studies | es_ES |
dc.title | Aryl piperazine and pyrrolidine as antimalarial agents. Synthesis and investigation of structure-activity relationships | es_ES |
dc.type | info:eu-repo/semantics/article | es_ES |
dc.identifier.doi | http://dx.doi.org/10.1016/j.exppara.2011.02.025 | es_ES |
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