Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties
Moraes, C.B., White, K.L., Braillard, S., Perez, C., Goo, J., Gaspar, L., Shackleford, D.M., Cordeiro-da-Silva, A., Thompson, R.C.A., Freitas-Junior, L., Charman, S.A. and Chatelain, E. (2015) Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties. Antimicrobial agents and chemotherapy, 59 (6). pp. 3645-3647.
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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.
|Publication Type:||Journal Article|
|Murdoch Affiliation:||School of Veterinary and Life Sciences|
|Publisher:||American Society for Microbiology|
|Copyright:||© 2015, American Society for Microbiology.|
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