Technology offer : Novel Synthetic Compounds for Treating Tropical Diseases
Three main groups of small molecules: two of them naturally occurring, chalcones and polyacetylenes, the other thieno[2,3-d] pyrimidines [Exo2], were found after phenotypic screening of small molecule libraries by high throughput cell imaging for their synthesis and biological activities targeting tuberculosis, malaria, leishmaniasis, and Chagas disease.
Using the results of the screening, University of Louisville (UofL) synthesized a series of chalcones and dihydrochalcones which were tested in Perou for their antiprotozoa activities against Leishmania amazonensis, Trypanosoma cruzi and Trypanosoma brucei. These tests have identified the minimum chemical requirements for the compounds to be active with strong potency and low cytotoxicity. UofL has also synthesized a series of Exo2 compounds, from which two of them showed high-selective and moderate-selective activities against Mycobacterium tuberculosis – including a multidrug resistant (MDR) strain with promising low cytotoxicity against normal cells.
Preclinical in vivo experiments were conducted which demonstrated high reduction of parasite burden. Furthermore, the candidate compounds did not exhibit any cutaneous toxicity at the tested doses.
Ref : OT-00074
Area of activity : HEALTH COSMETOLOGY
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