Issue 7, 2011
From the journal:

MedChemComm

Second generation analogues of RKA182: synthetic tetraoxanes with outstanding in vitro and in vivoantimalarial activities†

Francesc Marti,a   James Chadwick,a   Richard K. Amewu,a   Hollie Burrell-Saward,b   Abhishek Srivastava,c   Stephen A. Ward,c   Raman Sharma,a   Neil Berrya  and  Paul M. O'Neill*a  

* Corresponding authors

a Department of Chemistry, University of Liverpool, Liverpool, UK
E-mail: pmoneill@liverpool.ac.uk

b Department of Infectious and Tropical Disease, London School of Hygiene and Tropical Medicine, Keppel Street, London, UK

c Liverpool School of Tropical Medicine, Pembroke Place, Liverpool, UK

Abstract

A series of polar dispiro-1,2,4,5-tetraoxanes have been designed and synthesized by parallel synthesis. From this series, endoperoxides with activity as low as 0.2 nM have been obtained and representatives of this group have excellent oral activities in the P. bergheiANKA mouse model of malaria.

Graphical abstract: Second generation analogues of RKA182: synthetic tetraoxanes with outstanding in vitro and in vivoantimalarial activities

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Article information

DOI
https://doi.org/10.1039/C1MD00102G
Article type
Concise Article
Submitted
15 Apr 2011
Accepted
10 May 2011
First published
09 Jun 2011

Med. Chem. Commun., 2011,2, 661-665

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Second generation analogues of RKA182: synthetic tetraoxanes with outstanding in vitro and in vivoantimalarial activities

F. Marti, J. Chadwick, R. K. Amewu, H. Burrell-Saward, A. Srivastava, S. A. Ward, R. Sharma, N. Berry and P. M. O'Neill, Med. Chem. Commun., 2011, 2, 661 DOI: 10.1039/C1MD00102G

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