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The discovery,synthesis and antimalarial evaluation of natural product-based polyamine alkaloids |
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| Authors: | Vanida Choomuenwai Brett D. Schwartz Karren D. Beattie Katherine T. Andrews Shahan Khokhar Rohan A. Davis |
| Affiliation: | 1. Eskitis Institute, Griffith University, Brisbane, QLD 4111, Australia;2. Queensland Institute for Medical Research, Brisbane, QLD 4006, Australia |
| Abstract: | Bioassay-guided fractionation of an antimalarial extract derived from the fungus Ramaria subaurantiaca afforded the known polyamine alkaloid, pistillarin. Nine pistillarin analogues were synthesised via EDC-mediated chemistry and these compounds along with the previously reported natural product polyamines, ianthelliformisamines A–C and spermatinamine, were evaluated against Plasmodium falciparum (3D7) parasites and a normal human cell line to determine parasite-specific activity. Spermatinamine (IC50 0.23 μM) and pistillarin (IC50 1.9 μM) were the two most potent antimalarials identified during these studies. |
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