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http://hdl.handle.net/2445/65527
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DC Field | Value | Language |
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dc.contributor.author | Sola, Irene | - |
dc.contributor.author | Artigas, Albert | - |
dc.contributor.author | Taylor, Martin C. | - |
dc.contributor.author | Gbedema, Stephen Y. | - |
dc.contributor.author | Pérez Fernández, Belén | - |
dc.contributor.author | Clos, Victòria | - |
dc.contributor.author | Wright, Colin W. | - |
dc.contributor.author | Kelly, John M. | - |
dc.contributor.author | Muñoz-Torrero López-Ibarra, Diego | - |
dc.date.accessioned | 2015-05-13T12:15:32Z | - |
dc.date.available | 2015-05-13T12:15:32Z | - |
dc.date.issued | 2014-12-01 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | http://hdl.handle.net/2445/65527 | - |
dc.description.abstract | 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. | - |
dc.format.extent | 4 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Elsevier Ltd | - |
dc.relation.isformatof | Versió postprint del document publicat a: http://dx.doi.org/10.1016/j.bmcl.2014.10.025 | - |
dc.relation.ispartof | Bioorganic & Medicinal Chemistry Letters, 2014, vol. 24, num. 23, p. 5435-5438 | - |
dc.relation.uri | http://dx.doi.org/10.1016/j.bmcl.2014.10.025 | - |
dc.rights | (c) Elsevier Ltd, 2014 | - |
dc.source | Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) | - |
dc.subject.classification | Química orgànica | - |
dc.subject.classification | Química farmacèutica | - |
dc.subject.classification | Biologia molecular | - |
dc.subject.classification | Agents antiinfecciosos | - |
dc.subject.classification | Medicaments antipalúdics | - |
dc.subject.classification | Cervell | - |
dc.subject.classification | Permeabilitat | - |
dc.subject.other | Organic chemistry | - |
dc.subject.other | Pharmaceutical chemistry | - |
dc.subject.other | Molecular biology | - |
dc.subject.other | Anti-infective agents | - |
dc.subject.other | Antimalarials | - |
dc.subject.other | Brain | - |
dc.subject.other | Permeability | - |
dc.title | Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/acceptedVersion | - |
dc.identifier.idgrec | 644607 | - |
dc.date.updated | 2015-05-13T12:15:32Z | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
Appears in Collections: | Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) Articles publicats en revistes (Institut de Biomedicina (IBUB)) |
Files in This Item:
File | Description | Size | Format | |
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644607.pdf | 103.54 kB | Adobe PDF | View/Open |
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