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Issue 24, 2006
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Design and synthesis of orally active dispiro 1,2,4,5-tetraoxanes; synthetic antimalarials with superior activity to artemisinin

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Abstract

Unsymmetrical dispiro- and spirotetraoxanes have been designed and synthesized via acid-catalyzed cyclocondensation of bis(hydroperoxides) with ketones. Incorporation of water-soluble and polar functionalities, via reductive amination and amide bond formation, produces several analogues with low nanomolar in vitro antimalarial activity. Several analogues display an unprecedented level of oral antimalarial activity for this class of endoperoxide drug.

Graphical abstract: Design and synthesis of orally active dispiro 1,2,4,5-tetraoxanes; synthetic antimalarials with superior activity to artemisinin

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Publication details

The article was received on 18 Sep 2006, accepted on 26 Oct 2006 and first published on 03 Nov 2006


Article type: Communication
DOI: 10.1039/B613565J
Citation: Org. Biomol. Chem., 2006,4, 4431-4436
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    Design and synthesis of orally active dispiro 1,2,4,5-tetraoxanes; synthetic antimalarials with superior activity to artemisinin

    R. Amewu, A. V. Stachulski, S. A. Ward, N. G. Berry, P. G. Bray, J. Davies, G. Labat, L. Vivas and P. M. O'Neill, Org. Biomol. Chem., 2006, 4, 4431
    DOI: 10.1039/B613565J

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