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Elsevier, Bioorganic and Medicinal Chemistry Letters, 23(24), p. 5435-5438, 2014

DOI: 10.1016/j.bmcl.2014.10.025

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Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines

Journal article published in 2014 by Irene Sola, Albert Artigas ORCID, Martin C. Taylor, Stephen Y. Gbedema, Belén Pérez, M. Victòria Clos, M. Victòria Clos, Colin W. Wright, John M. Kelly, Diego Muñoz-Torrero ORCID,
This paper is available in a repository.
This paper is available in a repository.

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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.