• Publications
  • Influence
Antimalarial drug discovery: efficacy models for compound screening
TLDR
Different in vitro and in vivo screens for antimalarial drug discovery are suggested and a streamlined process for evaluating new compounds on the path from drug discovery to development is recommended.
Human African trypanosomiasis.
  • R. Brun, J. Blum
  • Medicine
    Infectious disease clinics of North America
  • 1 June 2012
Human African trypanosomiasis: pharmacological re‐engagement with a neglected disease
TLDR
The challenges of chemotherapy for human African trypanosomiasis (HAT) are discussed, and the few drugs registered for use against the disease are unsatisfactory for a number of reasons.
Antitrypanosomal and Antileishmanial Activities of Flavonoids and Their Analogues: In Vitro, In Vivo, Structure-Activity Relationship, and Quantitative Structure-Activity Relationship Studies
TLDR
A large set of flavonoid aglycones and glycosides were surveyed, as well as a panel of other related compounds of phenolic and phenylpropanoid nature, for their in vitro activities against Trypanosoma brucei rhodesiense, T. cruzi, and Leishmania donovani, and generally, the test compounds lacked cytotoxicity in vitro and in vivo.
Spiroindolones, a Potent Compound Class for the Treatment of Malaria
TLDR
The preclinical profile for an optimized spiroindolone drug candidate, NITD609, shows pharmacokinetic properties compatible with once-daily oral dosing and has single-dose efficacy in a rodent malaria model.
Kinetoplastids: related protozoan pathogens, different diseases.
Kinetoplastids are a group of flagellated protozoans that include the species Trypanosoma and Leishmania, which are human pathogens with devastating health and economic effects. The sequencing of the
...
...