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Please use this identifier to cite or link to this item: http://hdl.handle.net/123456789/10754

Title: Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines
Authors: Sola, Irene
Artigas, Albert
Taylor, Martin C.
Gbedema, Stephen Y.
Pérez, Belén
Clos, M. Victòria
Wright, Colin W.
Kelly, John M.
Muñoz-Torrero, Diego
Keywords: Molecular dimerization
Trypanocidal agents
Antimalarial agents
Bis(4-aminoquinolines)
Brain permeability
Issue Date: 2014
Publisher: Bioorganic & Medicinal Chemistry Letters
Citation: Bioorganic & Medicinal Chemistry Letters 24 (2014) 5435–5438
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.
Description: An article published by Bioorganic & Medicinal Chemistry Letters 24 (2014) 5435–5438
URI: http://hdl.handle.net/123456789/10754
Appears in Collections:College of Health Sciences

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