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Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines
Sola, Irene; Artigas, Albert; Taylor, Martin C.; Gbedema, Stephen Y.; Pérez Fernández, Belén; Clos Guillén, M. Victòria; Wright, Colin W.; Kelly, John M.; Muñoz-Torrero López-Ibarra, Diego
Universitat de Barcelona
We have synthesized a series of dimers of (+)-(7R,11R)-huprine Y and evaluated their activity against Trypanosoma brucei, Plasmodium falciparum, rat myoblast L6 cells and human acetylcholinesterase (hAChE), and their brain permeability. Most dimers have more potent and selective trypanocidal activity than huprine Y and are brain permeable, but they are devoid of antimalarial activity and remain active against hAChE. Lead optimization will focus on identifying compounds with a more favourable trypanocidal/anticholinesterase activity ratio.
Química orgànica
Química farmacèutica
Biologia molecular
Agents antiinfecciosos
Medicaments antipalúdics
Cervell
Permeabilitat
Organic chemistry
Pharmaceutical chemistry
Molecular biology
Anti-infective agents
Antimalarials
Brain
Permeability
(c) Elsevier Ltd, 2014
Article
info:eu-repo/semantics/acceptedVersion
Elsevier Ltd
         

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Sola, Irene; Artigas, Albert; Taylor, Martin C.; Gbedema, Stephen Y.; Pérez Fernández, Belén; Clos Guillén, M. Victòria; Wright, Colin W.; Kelly, John M.; Muñoz-Torrero López-Ibarra, Diego
Di Pietro, O.; Vicente García, Esther; Taylor, Martin C.; Berenguer, Diana; Viayna, Elisabet; Lanzoni, Anna; Sola, Irene; Sayago, Helena; Riera Lizandra, Ma. Cristina; Fisa Saladrigas, Roser; Clos Guillén, M. Victòria; Pérez Fernández, Belén; Kelly, John M.; Lavilla Grífols, Rodolfo; Muñoz-Torrero López-Ibarra, Diego
Di Pietro, O.; Vicente García, Esther; Taylor, Martin C.; Berenguer, Diana; Viayna, Elisabet; Lanzoni, Anna; Sola, Irene; Sayago, Helena; Riera Lizandra, Ma. Cristina; Fisa Saladrigas, Roser; Clos Guillén, M. Victòria; Pérez Fernández, Belén; Kelly, John M.; Lavilla Grífols, Rodolfo; Muñoz-Torrero López-Ibarra, Diego
Di Pietro, O.; Vicente García, Esther; Taylor, Martin C.; Berenguer, Diana; Viayna, Elisabet; Lanzoni, Anna; Sola, Irene; Sayago, Helena; Riera Lizandra, Ma. Cristina; Fisa Saladrigas, Roser; Clos Guillén, M. Victòria; Pérez Fernández, Belén; Kelly, John M.; Lavilla Grífols, Rodolfo; Muñoz-Torrero López-Ibarra, Diego
Viayna, Elisabet; Sola, Irene; Bartolini, Manuela; De Simone, A.; Tapia-Rojas, C.; Serrano, Felipe G.; Sabaté Lagunas, Raimon; Juárez-Jiménez, Jordi; Pérez Fernández, Belén; Luque Garriga, F. Xavier; Andrisano, Vincenza; Clos Guillén, M. Victòria; Inestrosa, Nibaldo C.; Muñoz-Torrero López-Ibarra, Diego
 

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