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dc.contributor.authorSola, I.*
dc.contributor.authorArtigas, A.*
dc.contributor.authorTaylor, M.C.*
dc.contributor.authorGbedema, Stephen Y.*
dc.contributor.authorPerez, B.*
dc.contributor.authorClos, M.V.*
dc.contributor.authorWright, Colin W.*
dc.contributor.authorKelly, J.M.*
dc.contributor.authorMuñoz-Torrero, D.*
dc.date.accessioned2015-12-04T15:28:39Z
dc.date.available2015-12-04T15:28:39Z
dc.date.issued2014-12
dc.identifier.citationSola I, Artigas A, Taylor MC et al (2014) Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines. Bioorganic & Medicinal Chemistry Letters, 24(23): 5435-5438.en_US
dc.identifier.urihttp://hdl.handle.net/10454/7496
dc.description.abstractWe 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.en_US
dc.language.isoenen_US
dc.relation.isreferencedbyhttp://dx.doi.org/10.1016/j.bmcl.2014.10.025en_US
dc.rights© 2014 Elsevier. Reproduced in accordance with the publisher's self-archiving policy. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/
dc.subjectMolecular dimerization; Trypanocidal agents; Antimalarial agents; Bis(4-aminoquinolines); Brain permeabilityen_US
dc.titleSynthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines.en_US
dc.status.refereedyesen_US
dc.date.application2014-10-27
dc.typeArticleen_US
dc.type.versionAccepted Manuscripten_US
refterms.dateFOA2018-07-25T13:16:55Z


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