Universidad Peruana Cayetano Heredia

Aryl piperazine and pyrrolidine as antimalarial agents. Synthesis and investigation of structure-activity relationships

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dc.contributor.author Mendoza, A.
dc.contributor.author Pérez-Silanes, S.
dc.contributor.author Quiliano, M.
dc.contributor.author Pabón, A.
dc.contributor.author Galiano, S.
dc.contributor.author González, G.
dc.contributor.author Garavito, G.
dc.contributor.author Zimic-Peralta, Mirko Juan
dc.contributor.author Vaisberg Wollach, Abraham Jaime
dc.contributor.author Aldana, I.
dc.contributor.author Monge, A.
dc.contributor.author Deharo, E.
dc.date.accessioned 2022-01-18T19:26:46Z
dc.date.available 2022-01-18T19:26:46Z
dc.date.issued 2011
dc.identifier.uri https://hdl.handle.net/20.500.12866/10854
dc.description.abstract Piperazine and pyrrolidine derivatives were synthesised 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 ≤10μM. The most active compound 1-(4-fluoronaphthyl)-3-[4-(4-nitro-2-trifluoromethylphenyl)piperazin-1-yl] propan-1-ol was almost 20-40 times more active on P. falciparum (IC50: 0.5μM) than on tumorogenic and non-tumorogenic cells. In vivo it has a very weak effect; inhibiting 35% of parasite growth only, at 10mg/kg/day against Plasmodium berghei infected mice without any impact on survival time. In silico molecular docking study and molecular electrostatic potential calculation revealed that this compound bound to the active site of Plasmodium plasmepsin II enzyme. en_US
dc.language.iso eng
dc.publisher Elsevier
dc.relation.ispartofseries Experimental Parasitology
dc.rights info:eu-repo/semantics/restrictedAccess
dc.rights.uri https://creativecommons.org/licenses/by-nc-nd/4.0/deed.es
dc.subject Humans en_US
dc.subject Controlled Study en_US
dc.subject Unclassified Drug en_US
dc.subject Plasmodium Falciparum en_US
dc.subject Antimalarial Agent en_US
dc.subject Chloroquine en_US
dc.subject Cell Line en_US
dc.subject Doxycycline en_US
dc.subject Antimalarials en_US
dc.subject Host Parasite Interaction en_US
dc.subject Parasite Development en_US
dc.subject Protozoal DNA en_US
dc.subject Monotherapy en_US
dc.subject Developmental Stage en_US
dc.subject Plant Extracts en_US
dc.subject Cell Proliferation en_US
dc.subject Antimalarial Activity en_US
dc.subject Combination Chemotherapy en_US
dc.subject Trophozoite en_US
dc.subject Artemether en_US
dc.subject Inhibitory Concentration 50 en_US
dc.subject Amodiaquine en_US
dc.subject Apoptosis en_US
dc.subject Atovaquone en_US
dc.subject Bruceantin en_US
dc.subject Brusatol en_US
dc.subject Cell Death en_US
dc.subject Cell Membrane Permeability en_US
dc.subject DNA Replication en_US
dc.subject Erythrocyte Membrane en_US
dc.subject Erythrocytes en_US
dc.subject Halofantrine en_US
dc.subject Heme en_US
dc.subject Lymphoblast en_US
dc.subject Mefloquine en_US
dc.subject Plant Medicinal Product en_US
dc.subject Plasmodium Yoelii en_US
dc.subject Quassia Amara en_US
dc.subject Quassinoid en_US
dc.subject Simalikalactone D en_US
dc.subject Simaroubaceae en_US
dc.title Aryl piperazine and pyrrolidine as antimalarial agents. Synthesis and investigation of structure-activity relationships en_US
dc.type info:eu-repo/semantics/article
dc.identifier.doi https://doi.org/10.1016/j.exppara.2011.02.025
dc.subject.ocde https://purl.org/pe-repo/ocde/ford#3.03.07
dc.relation.issn 1090-2449


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