| Promising Aculeatin Derivatives |
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New Weapons against Malaria Aculeatins belong to a novel family of molecules recently isolated from the plant Amonum aculeatum commonly used in Papua New Guinea as a traditional medicine to treat fever and malaria. Researchers at the Molecular Pharmacochemistry department, University Joseph Fourier, have developed a unique synthesis pathway giving access to a wide range of aculeatin derivatives. This highly flexible diversity-oriented approach enables the synthesis of numerous and complex derivatives, some of which already demonstrate enhanced anti-plasmodium activities and reduced cell toxicity. This new method of synthesis can result in opportunities regarding both the molecular optimization of aculeatins, as well as an understanding of their mode of action. Key features
Benefits The technology has the potential to produce a wide range of derivatives, enabling a clear understanding of structure-activity relationships (SAR). By establishing a critical mass where sufficient numbers of molecules are available, followed by an in-depth analysis of the structure-activity relationship, the identification ol lead compounds is made possible.
The Plasmodium falciparum parasite causes Malaria, one of the world's most common infectious disease killing over one million people each year, mainly in sub-tropical climates. Key laboratory results
- IC50 on Plasmodium falciparum as low as 80-90nM - IC50 on Toxoplasma gondii under 180nM
Intellectual Property Covered by French Patent # 07/06929 (October 3, 2007) Technology Status Floralis is currently looking for partners to further develop this exciting technology which demonstrates significant potential in the development og highly promising molecules with malaria inhibiting properties. Contacts Mathieu TILQUIN
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| "Thanks to the Optical Imaging Platform we have been able to carry out preliminary trials" JS Sun, DNA Therapeutics |
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