TY - JOUR
T1 - Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties
AU - Moraes, Carolina B
AU - White, Karen L
AU - Braillard, Stephanie
AU - Perez, Catherine
AU - Goo, Junghyun
AU - Gaspar, Luis
AU - Shackleford, David M
AU - Cordeiro-da-Silva, Anabela
AU - Thompson, R C Andrew
AU - Freitas-Junior, Lucio H
AU - Charman, Susan A
AU - Chatelain, Eric
PY - 2015
Y1 - 2015
N2 - 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.
AB - 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.
UR - http://aac.asm.org.ezproxy.lib.monash.edu.au/content/59/6/3645.full.pdf+html
U2 - 10.1128/AAC.05139-14
DO - 10.1128/AAC.05139-14
M3 - Article
SN - 0066-4804
VL - 59
SP - 3645
EP - 3647
JO - Antimicrobial Agents and Chemotherapy
JF - Antimicrobial Agents and Chemotherapy
IS - 6
ER -
