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Identification and characterization of a novel flavin-containing spermine oxidase of mammalian cell origin.
TLDR
The data indicate that the enzyme represents a novel mammalian oxidase which, on the basis of substrate specificity, is designated spermine oxidase in order to distinguish it from the PAO involved in polyamine back-conversion.
SCYX-7158, an Orally-Active Benzoxaborole for the Treatment of Stage 2 Human African Trypanosomiasis
TLDR
The biological and pharmacokinetic properties of SCYX-7158 suggest that this compound will be efficacious and safe to treat stage 2 HAT, and is selected to enter preclinical studies, with expected progression to phase 1 clinical trials in 2011.
Polyamine metabolism: a potential therapeutic target in trypanosomes.
TLDR
alpha-Difluoromethylornithine (RMI 71,782), a specific irreversible inhibitor of the first step in polyamine biosynthesis, cures mice infected with a virulent, rodent-passaged strain of Trypanosoma brucei bruceo, drawing attention to polyamine metabolism as a target for chemotherapy of parasitic diseases.
In vivo effects of difluoromethylornithine on trypanothione and polyamine levels in bloodstream forms of Trypanosoma brucei.
TLDR
Depletion of this metabolite may be an important contributory factor to the selective toxic effect of DFMO, particularly in its synergistic effect with other trypanocidal drugs.
Inducible Resistance to Oxidant Stress in the Protozoan Leishmania chagasi *
TLDR
It is concluded that leishmania have redundant mechanisms for resisting toxic oxidants, some are induced during developmental change and others are induced in response to environmental stress.
Chemotherapy of Human African Trypanosomiasis
  • C. Bacchi
  • Medicine
    Interdisciplinary perspectives on infectious…
  • 20 August 2009
TLDR
This article presents an update of classic chemotherapeutic agents, in use for >50 years and the recent development of promising non-toxic combination chemotherapy suitable for use in rural clinics.
Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity.
TLDR
A series of polyaminoguanidines and polyaminobiguanides were synthesized and evaluated as potential antitrypanosomal agents and the most effective analogues inhibited parasitic growth in vitro with IC50 values of 0.09 and 0.18 microM, respectively.
Benzoxaboroles: a new class of potential drugs for human African trypanosomiasis.
TLDR
A series of benzoxaborole-6-carboxamides is discovered and optimized to provide trypanocidal compounds that are orally active in murine models of human African trypanosomiasis and the in vivo pharmacokinetic properties of lead compounds from the series are reported.
Subcellular Localization of the Enzymes of the Arginine Dihydrolase Pathway in Trichomonas vaginalis and Tritrichomonas foetus
TLDR
The results demonstrate the presence of theArginine dihydrolase pathway in T. foetus and indicate that at least a portion of the arginine deiminase in trichomonads is membrane associated.
Pharmacokinetics and pharmacodynamics utilizing unbound target tissue exposure as part of a disposition-based rationale for lead optimization of benzoxaboroles in the treatment of Stage 2 Human
TLDR
A progression strategy for the discovery of new anti-parasitic drugs that uses in vitro susceptibility, time-kill and reversibility measures to define the therapeutically relevant exposure required in target tissues of animal infection models is presented.
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