Title:
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Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines
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Author:
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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
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Other authors:
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Universitat de Barcelona |
Abstract:
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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. |
Subject(s):
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-Química orgànica -Química farmacèutica -Biologia molecular -Agents antiinfecciosos -Medicaments antipalúdics -Cervell -Permeabilitat -Organic chemistry -Pharmaceutical chemistry -Molecular biology -Anti-infective agents -Antimalarials -Brain -Permeability |
Rights:
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(c) Elsevier Ltd, 2014
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Document type:
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Article Article - Accepted version |
Published by:
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Elsevier Ltd
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