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2014-12-01

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Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/65527

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

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http://dx.doi.org/10.1016/j.bmcl.2014.10.025

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.

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Química orgànica, Química farmacèutica, Biologia molecular, Agents antiinfecciosos, Medicaments antipalúdics, Cervell, Permeabilitat

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Organic chemistry, Pharmaceutical chemistry, Molecular biology, Anti-infective agents, Antimalarials, Brain, Permeability

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Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)
Articles publicats en revistes (Institut de Biomedicina (IBUB))

Citation

SOLA, Irene, et al. Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines. Bioorganic & Medicinal Chemistry Letters. 2014. Vol. 24, num. 23, pags. 5435-5438. ISSN 0960-894X. [consulted: 16 of June of 2026]. Available at: https://hdl.handle.net/2445/65527

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