Loading...
Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines.
Sola, I. Artigas, A. Taylor, M.C. Gbedema, Stephen Y. Perez, B. Clos, M.V. Wright, Colin W. Kelly, J.M. Muñoz-Torrero, D.
Sola, I.
Artigas, A.
Taylor, M.C.
Gbedema, Stephen Y.
Perez, B.
Clos, M.V.
Wright, Colin W.
Kelly, J.M.
Muñoz-Torrero, D.
Publication Date
2014-12
End of Embargo
Supervisor
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/
Peer-Reviewed
Yes
Open Access status
openAccess
Accepted for publication
Institution
Department
Awarded
Embargo end date
Collections
Additional title
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.
Version
Accepted manuscript
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.
Link to publisher’s version
Link to published version
Link to Version of Record
Type
Article