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Identification of a 1,2,4,5‐Tetraoxane Antimalarial Drug‐Development Candidate (RKA 182) with Superior Properties to the Semisynthetic Artemisinins
Author(s) -
O'Neill Paul M.,
Amewu Richard K.,
Nixon Gemma L.,
Bousejra ElGarah Fatima,
Mungthin Mathirut,
Chadwick James,
Shone Alison E.,
Vivas Livia,
Lander Hollie,
Barton Victoria,
Muangnoicharoen Sant,
Bray Patrick G.,
Davies Jill,
Park B. Kevin,
Wittlin Sergio,
Brun Reto,
Preschel Michael,
Zhang Kesheng,
Ward Stephen A.
Publication year - 2010
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201001026
Subject(s) - artemisinin , drug , drug candidate , pharmacology , identification (biology) , malaria , plasmodium falciparum , medicine , traditional medicine , biology , immunology , botany
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.