Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties

C.B. Moraes; K.L. White; S. Braillard; C. Perez; J. Goo; L. Gaspar; D.M. Shackleford; A. Cordeiro-da-Silva; R.C.A. Thompson; L. Freitas-Junior; S.A. Charman; E. Chatelain

doi:10.1128/AAC.05139-14

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Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties

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Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties

C.B. Moraes, K.L. White, S. Braillard, C. Perez, J. Goo, L. Gaspar, D.M. Shackleford, A. Cordeiro-da-Silva, R.C.A. Thompson, L. Freitas-Junior, …

Antimicrobial agents and chemotherapy, Vol.59(6), pp.3645-3647

2015

DOI: https://doi.org/10.1128/AAC.05139-14

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Abstract

With the aim of improving the available drugs for the treatment of Chagas disease, individual enantiomers of nifurtimox were characterized. The results indicate that the enantiomers are equivalent in their in vitro activity against a panel of Trypanosoma cruzi strains; in vivo efficacy in a murine model of Chagas disease; in vitro toxicity and absorption, distribution, metabolism, and excretion characteristics; and in vivo pharmacokinetic properties. There is unlikely to be any therapeutic benefit of an individual nifurtimox enantiomer over the racemic mixture.

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Title: Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties
Authors/Creators: C.B. Moraes (Author/Creator) - Institut Pasteur Korea
K.L. White (Author/Creator) - Monash University
S. Braillard (Author/Creator) - Drugs for Neglected Diseases Initiative
C. Perez (Author/Creator) - Murdoch University
J. Goo (Author/Creator) - Institut Pasteur Korea
L. Gaspar (Author/Creator) - Institut Pasteur Korea
D.M. Shackleford (Author/Creator) - Monash University
A. Cordeiro-da-Silva (Author/Creator) - Instituto de Biologia Molecular e Celular
R.C.A. Thompson (Author/Creator)
L. Freitas-Junior (Author/Creator) - Institut Pasteur Korea
S.A. Charman (Author/Creator) - Monash University
E. Chatelain (Author/Creator) - Drugs for Neglected Diseases Initiative
Publication Details: Antimicrobial agents and chemotherapy, Vol.59(6), pp.3645-3647
Publisher: American Society for Microbiology
Identifiers: 991005545226707891
Copyright: © 2015, American Society for Microbiology.
Murdoch Affiliation: School of Veterinary and Life Sciences
Language: English
Resource Type: Journal article

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Collaboration types: Domestic collaboration; International collaboration
Citation topics: 1 Clinical & Life Sciences; 1.261 Parasitology - Trypanosoma & Leishmania; 1.261.596 Trypanosoma Biology
Web Of Science research areas: Microbiology; Pharmacology & Pharmacy
ESI research areas: Pharmacology & Toxicology