Identification of a 1,2,4,5-Tetraoxane Antimalarial Drug-Development Candidate (RKA 182) with Superior Properties to the Semisynthetic Artemisinins (pages 5693–5697)
Paul M. O'Neill, Richard K. Amewu, Gemma L. Nixon, Fatima Bousejra ElGarah, Mathirut Mungthin, James Chadwick, Alison E. Shone, Livia Vivas, Hollie Lander, Victoria Barton, Sant Muangnoicharoen, Patrick G. Bray, Jill Davies, B. Kevin Park, Sergio Wittlin, Reto Brun, Michael Preschel, Kesheng Zhang and Stephen A. Ward
Version of Record online: 13 JUL 2010 | DOI: 10.1002/anie.201001026
Fighting drug resistence: From a library of over 150 1,2,4,5-tetraoxanes, the candidate RKA 182 was selected for preclinical development as an antimalarial agent. RKA 182 has outstanding in vitro activity against resistant strains of P. falciparum and retains this level of activity against southeast asian isolates that failed artemisinin-based combination therapy.