Identification of a 1,2,4,5-tetraoxane antimalarial drug-development candidate (RKA 182) with superior properties to the semisynthetic artemisinins

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; Stephen A. Ward

doi:10.1002/anie.201001026

Identification of a 1,2,4,5-tetraoxane antimalarial drug-development candidate (RKA 182) with superior properties to the semisynthetic artemisinins

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, Stephen A. Ward

Research output: Contribution to journal › Article › peer-review

117 Citations (Scopus)

Abstract

(Figure Presented) Fighting drug resistence: From a library of over 150 1,2,4,5-tetraoxanes, the candidate RKA182 was selected for preclinical development as an antimalarial agent. RKA182 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.

Original language	English
Pages (from-to)	5693-5697
Number of pages	5
Journal	Angewandte Chemie - International Edition
Volume	49
Issue number	33
DOIs	https://doi.org/10.1002/anie.201001026
Publication status	Published - 2 Aug 2010
Externally published	Yes

Keywords

Antimalarial agents
Drug development
Endoperoxides
Medicinal chemistry
Tetraoxanes

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10.1002/anie.201001026

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O'Neill, P. M., Amewu, R. K., Nixon, G. L., ElGarah, F. B., Mungthin, M., Chadwick, J., Shone, A. E., Vivas, L., Lander, H., Barton, V., Muangnoicharoen, S., Bray, P. G., Davies, J., Park, B. K., Wittlin, S., Brun, R., Preschel, M., Zhang, K., & Ward, S. A. (2010). Identification of a 1,2,4,5-tetraoxane antimalarial drug-development candidate (RKA 182) with superior properties to the semisynthetic artemisinins. Angewandte Chemie - International Edition, 49(33), 5693-5697. https://doi.org/10.1002/anie.201001026

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title = "Identification of a 1,2,4,5-tetraoxane antimalarial drug-development candidate (RKA 182) with superior properties to the semisynthetic artemisinins",

abstract = "(Figure Presented) Fighting drug resistence: From a library of over 150 1,2,4,5-tetraoxanes, the candidate RKA182 was selected for preclinical development as an antimalarial agent. RKA182 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.",

keywords = "Antimalarial agents, Drug development, Endoperoxides, Medicinal chemistry, Tetraoxanes",

author = "O'Neill, {Paul M.} and Amewu, {Richard K.} and Nixon, {Gemma L.} and ElGarah, {Fatima Bousejra} and Mathirut Mungthin and James Chadwick and Shone, {Alison E.} and Livia Vivas and Hollie Lander and Victoria Barton and Sant Muangnoicharoen and Bray, {Patrick G.} and Jill Davies and Park, {B. Kevin} and Sergio Wittlin and Reto Brun and Michael Preschel and Kesheng Zhang and Ward, {Stephen A.}",

year = "2010",

month = aug,

day = "2",

doi = "10.1002/anie.201001026",

language = "English",

volume = "49",

pages = "5693--5697",

journal = "Angewandte Chemie - International Edition",

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O'Neill, PM, Amewu, RK, Nixon, GL, ElGarah, FB, Mungthin, M, Chadwick, J, Shone, AE, Vivas, L, Lander, H, Barton, V, Muangnoicharoen, S, Bray, PG, Davies, J, Park, BK, Wittlin, S, Brun, R, Preschel, M, Zhang, K & Ward, SA 2010, 'Identification of a 1,2,4,5-tetraoxane antimalarial drug-development candidate (RKA 182) with superior properties to the semisynthetic artemisinins', Angewandte Chemie - International Edition, vol. 49, no. 33, pp. 5693-5697. https://doi.org/10.1002/anie.201001026

TY - JOUR

T1 - Identification of a 1,2,4,5-tetraoxane antimalarial drug-development candidate (RKA 182) with superior properties to the semisynthetic artemisinins

AU - O'Neill, Paul M.

AU - Amewu, Richard K.

AU - Nixon, Gemma L.

AU - ElGarah, Fatima Bousejra

AU - Mungthin, Mathirut

AU - Chadwick, James

AU - Shone, Alison E.

AU - Vivas, Livia

AU - Lander, Hollie

AU - Barton, Victoria

AU - Muangnoicharoen, Sant

AU - Bray, Patrick G.

AU - Davies, Jill

AU - Park, B. Kevin

AU - Wittlin, Sergio

AU - Brun, Reto

AU - Preschel, Michael

AU - Zhang, Kesheng

AU - Ward, Stephen A.

PY - 2010/8/2

Y1 - 2010/8/2

N2 - (Figure Presented) Fighting drug resistence: From a library of over 150 1,2,4,5-tetraoxanes, the candidate RKA182 was selected for preclinical development as an antimalarial agent. RKA182 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.

AB - (Figure Presented) Fighting drug resistence: From a library of over 150 1,2,4,5-tetraoxanes, the candidate RKA182 was selected for preclinical development as an antimalarial agent. RKA182 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.

KW - Antimalarial agents

KW - Drug development

KW - Endoperoxides

KW - Medicinal chemistry

KW - Tetraoxanes

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U2 - 10.1002/anie.201001026

DO - 10.1002/anie.201001026

M3 - Article

C2 - 20629058

AN - SCOPUS:77955336999

SN - 1433-7851

VL - 49

SP - 5693

EP - 5697

JO - Angewandte Chemie - International Edition

JF - Angewandte Chemie - International Edition

IS - 33

ER -

Identification of a 1,2,4,5-tetraoxane antimalarial drug-development candidate (RKA 182) with superior properties to the semisynthetic artemisinins

Abstract

Keywords

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