Synthesis of RKA 182

P. M. O’Neill et al.

doi:10.1055/s-0030-1258710

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Synfacts 2010(11): 1220-1220
DOI: 10.1055/s-0030-1258710

Synthesis of Natural Products and Potential Drugs

Synthesis of RKA 182

Contributor(s): Philip Kocienski
P. M. O’Neill et al.*
University of Liverpool, Liverpool School of Tropical Medicine, London School of Hygiene and Tropical Medicine, UK; Phramongkutklao College of Medicine, Bangkok, Thailand; Swiss Tropical and Public Health Institute, Basel and Carbogen AMCIS, Hunzenschwil, Switzerland

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Publication History

Publication Date:
21 October 2010 (online)

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Significance

RK 182 is a remarkably stable, orally available antimalarial agent selected for development from a library of over one hundred and fifty 1,2,4,5-tetraoxane analogues. As the water-soluble ditosylate salt, RKA 182, displayed an IC₅₀ of 0.87 nM and an ED₅₀/ED₉₀ of 1.1/4.1 mg kg^-¹, which is superior to the leading synthetic artemisinin analogues currently in phase II development. It also shows a long duration of action with 79% being recovered after four hours in infected blood.