Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines.
dc.contributor.author | Sola, I. | * |
dc.contributor.author | Artigas, A. | * |
dc.contributor.author | Taylor, M.C. | * |
dc.contributor.author | Gbedema, Stephen Y. | * |
dc.contributor.author | Perez, B. | * |
dc.contributor.author | Clos, M.V. | * |
dc.contributor.author | Wright, Colin W. | * |
dc.contributor.author | Kelly, J.M. | * |
dc.contributor.author | Muñoz-Torrero, D. | * |
dc.date.accessioned | 2015-12-04T15:28:39Z | |
dc.date.available | 2015-12-04T15:28:39Z | |
dc.date.issued | 2014-12 | |
dc.identifier.citation | Sola 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.uri | http://hdl.handle.net/10454/7496 | |
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. | en_US |
dc.language.iso | en | en_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.subject | Molecular dimerization; Trypanocidal agents; Antimalarial agents; Bis(4-aminoquinolines); Brain permeability | en_US |
dc.title | Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines. | en_US |
dc.status.refereed | yes | en_US |
dc.date.application | 2014-10-27 | |
dc.type | Article | en_US |
dc.type.version | Accepted Manuscript | en_US |
dc.identifier.doi | https://doi.org/10.1016/j.bmcl.2014.10.025 | |
refterms.dateFOA | 2018-07-25T13:16:55Z |