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http://hdl.handle.net/2445/65527| 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, Victòria Wright, Colin W. Kelly, John M. Muñoz-Torrero López-Ibarra, Diego |
| Keywords: | Química orgànica Química farmacèutica Biologia molecular Agents antiinfecciosos Medicaments antipalúdics Cervell Permeabilitat Organic chemistry Pharmaceutical chemistry Molecular biology Anti-infective agents Antimalarials Brain Permeability |
| 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: http://dx.doi.org/10.1016/j.bmcl.2014.10.025 |
| It is part of: | Bioorganic & Medicinal Chemistry Letters, 2014, vol. 24, num. 23, p. 5435-5438 |
| URI: | http://hdl.handle.net/2445/65527 |
| Related resource: | http://dx.doi.org/10.1016/j.bmcl.2014.10.025 |
| 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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