Investigation of Indolglyoxamide and Indolacetamide Analogues of Polyamines as Antimalarial and Antitrypanosomal Agents

  title={Investigation of Indolglyoxamide and Indolacetamide Analogues of Polyamines as Antimalarial and Antitrypanosomal Agents},
  author={J. Wang and M. Kaiser and B. Copp},
  journal={Marine Drugs},
  pages={3138 - 3160}
  • J. Wang, M. Kaiser, B. Copp
  • Published 2014
  • Biology, Medicine
  • Marine Drugs
  • Pure compound screening has previously identified the indolglyoxylamidospermidine ascidian metabolites didemnidine A and B (2 and 3) to be weak growth inhibitors of Trypanosoma brucei rhodesiense (IC50 59 and 44 μM, respectively) and Plasmodium falciparum (K1 dual drug resistant strain) (IC50 41 and 15 μM, respectively), but lacking in selectivity (L6 rat myoblast, IC50 24 μM and 25 μM, respectively). To expand the structure–activity relationship of this compound class towards both parasites… CONTINUE READING
    12 Citations
    Synthesis and antimalarial evaluation of artesunate-polyamine and trioxolane-polyamine conjugates.
    • 6
    Exploration of the antibiotic potentiating activity of indolglyoxylpolyamines.
    • 2
    Study of the antimalarial properties of hydroxyethylamine derivatives using green fluorescent protein transformed Plasmodium berghei
    • 1
    • PDF
    Polyamine-based analogs and conjugates as antikinetoplastid agents.
    • 9
    Origins and Bioactivities of Natural Compounds Derived from Marine Ascidians and Their Symbionts
    • 8
    • PDF
    Uptake and metabolism of arginine impact Plasmodium development in the liver
    • 11
    • PDF


    Synthesis and in vitro and in vivo evaluation of antimalarial polyamines.
    • 14
    Discovery and preliminary structure-activity relationship analysis of 1,14-sperminediphenylacetamides as potent and selective antimalarial lead compounds.
    • 14
    Antimalarial polyamine analogues.
    • 33
    Synthesis and biological evaluation of s-triazine substituted polyamines as potential new anti-trypanosomal drugs.
    • 106
    • Highly Influential
    Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity.
    • 49