Evidence for a Common Non??Heme Chelatable??Iron??Dependent Activation Mechanism for Semisynthetic and Synthetic Endoperoxide Antimalarial Drugs

…, VE Barton, M Al??Helal, M Jones…

Index: Stocks, Paul A.; Bray, Patrick G.; Barton, Victoria E.; Al-Helal, Mohammed; Jones, Michael; Araujo, Nuna C.; Gibbons, Peter; Ward, Stephen A.; Hughes, Ruth H.; Biagini, Giancarlo A.; Davies, Jill; Amewu, Richard; Mercer, Amy E.; Ellis, Gemma; O'Neill, Paul M. Angewandte Chemie - International Edition, 2007 , vol. 46, # 33 p. 6278 - 6283

Full Text: HTML

Citation Number: 85

Abstract

Herbal extracts of Artemisia annua have been used to treat malaria since ancient times. Artemisinin (1), the refined natural product, is extremely potent and displays little or no cross- resistance with other antimalarial compounds.[1, 2] However, it is relatively expensive, has poor bioavailability, and has poor pharmacokinetics, properties that are shared by semisynthetic derivatives such as artesunate (2) and artemether (3).[3, 4] Recently, the ...