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


Marti, F; Chadwick, J; Amewu, RK; Burrell-Saward, H; Srivastava, A; Ward, SA; Sharma, R; Berry, N; O'Neill, PM; Se, DA; (2011) Second generation analogues of RKA182: synthetic tetraoxanes with outstanding in vitro and in vivo antimalarial activities. MedChemComm, 2 (7). pp. 661-665. ISSN 2040-2503 DOI: https://doi.org/10.1039/c1md00102g

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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. berghei ANKA mouse model of malaria.

Item Type: Article
Keywords: drug-development candidate, crystal-structure, dispiro-1, 2, 4, 5-tetraoxanes, artemisinin, peroxides, spiro-1, 2, 4, 5-tetraoxacycloalkanes, 1, 2, 4, 5-tetraoxane, identification, mechanism, malaria
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Immunology and Infection
Research Centre: Malaria Centre
URI: http://researchonline.lshtm.ac.uk/id/eprint/121

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