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Title: Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines
Author: Sola, Irene
Artigas, Albert
Taylor, Martin C.
Gbedema, Stephen Y.
Pérez Fernández, Belén
Clos Guillén, M. Victòria
Wright, Colin W.
Kelly, John M.
Muñoz-Torrero López-Ibarra, Diego
Keywords: Química orgànica
Química farmacèutica
Biologia molecular
Agents antiinfecciosos
Medicaments antipalúdics
Organic chemistry
Pharmaceutical chemistry
Molecular biology
Anti-infective agents
Issue Date: 1-Dec-2014
Publisher: Elsevier Ltd
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.
Note: Versió postprint del document publicat a:
It is part of: Bioorganic & Medicinal Chemistry Letters, 2014, vol. 24, num. 23, p. 5435-5438
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ISSN: 0960-894X
Appears in Collections:Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)
Articles publicats en revistes (Institut de Biomedicina (IBUB))

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